Lapatinib-d5(Synonyms: GW572016-d5; GW2016-d5)

发表于2024年10月30日由上海金畔生物科技有限公司

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

Lapatinib-d5 (Synonyms: GW572016-d5; GW2016-d5)

Lapatinib-d5 是 Lapatinib 氘代物。Lapatinib (GW572016) 是一种 ErbB-2 和 EGFR 酪氨酸激酶结构域的有效抑制剂，对纯化的 EGFR 和 ErbB-2 的 IC₅₀ 值分别为 10.2 和 9.8 nM。

Lapatinib-d5 Chemical Structure

CAS No. : 2748212-14-6

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生物活性	Lapatinib-d5 is deuterium labeled Lapatinib. Lapatinib (GW572016) is a potent inhibitor of the ErbB-2 and EGFR tyrosine kinase domains with IC50 values against purified EGFR and ErbB-2 of 10.2 and 9.8 nM, respectively^[1].
体外研究 (In Vitro)	Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs^[1]. Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量	586.09
Formula	C₂₉H₂₁D₅ClFN₄O₄S
CAS 号	2748212-14-6
运输条件	Room temperature in continental US; may vary elsewhere.
储存方式	Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献	[1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216. [2]. Rusnak DW, et al. The effects of the novel, reversible epidermal growth factor receptor/ErbB-2 tyrosine kinase inhibitor, GW2016, on the growth of human normal and tumor-derived cell lines in vitro and in vivo. Mol Cancer Ther. 2001 Dec;1(2):85-94

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Lapatinib-d4-1(Synonyms: GW572016-d4-1; GW2016-d4-1)

发表于2024年10月30日由上海金畔生物科技有限公司

Lapatinib-d4-1 (Synonyms: GW572016-d4-1; GW2016-d4-1)

Lapatinib-d4-1 是 Lapatinib 氘代物。Lapatinib (GW572016) 是一种 ErbB-2 和 EGFR 酪氨酸激酶结构域的有效抑制剂，对纯化的 EGFR 和 ErbB-2 的 IC₅₀ 值分别为 10.2 和 9.8 nM。

Lapatinib-d4-1 Chemical Structure

CAS No. : 1184264-15-0

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生物活性	Lapatinib-d4-1 is deuterium labeled Lapatinib. Lapatinib (GW572016) is a potent inhibitor of the ErbB-2 and EGFR tyrosine kinase domains with IC50 values against purified EGFR and ErbB-2 of 10.2 and 9.8 nM, respectively^[1].
体外研究 (In Vitro)	Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs^[1]. Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量	585.08
Formula	C₂₉H₂₂D₄ClFN₄O₄S
CAS 号	1184264-15-0
运输条件	Room temperature in continental US; may vary elsewhere.
储存方式	Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献	[1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216. [2]. Rusnak DW, et al. The effects of the novel, reversible epidermal growth factor receptor/ErbB-2 tyrosine kinase inhibitor, GW2016, on the growth of human normal and tumor-derived cell lines in vitro and in vivo. Mol Cancer Ther. 2001 Dec;1(2):85-94

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GW9662

发表于2024年10月24日由上海金畔生物科技有限公司

GW9662 纯度: 99.83%

GW9662是有效，选择性的 PPARγ 拮抗剂，IC₅₀值为3.3 nM，比PPARα和PPARδ的选择性高10倍和1000倍。

GW9662 Chemical Structure

CAS No. : 22978-25-2

规格	价格	是否有货
Free Sample (0.1-0.5 mg)		Apply now
10 mM * 1 mL in DMSO	￥656	In-stock
5 mg	￥596	In-stock
10 mg	￥900	In-stock
25 mg	￥1400	In-stock
50 mg	￥2300	In-stock
100 mg	￥4000	In-stock
200 mg		询价
500 mg		询价

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GW9662 相关产品

•相关化合物库:

Bioactive Compound Library Plus
Cell Cycle/DNA Damage Compound Library
Anti-Cancer Compound Library
Anti-Aging Compound Library
Transcription Factor Targeted Library
Lipid Metabolism Compound Library

生物活性

GW9662 is a potent and selective PPARγ antagonist with an IC₅₀ of 3.3 nM, showing 10 and 1000-fold selectivity over PPARα and PPARδ, respectively.

IC₅₀ & Target^[1]

PPARγ

3.3 nM (IC₅₀)

PPARα

32 nM (IC₅₀)

PPARδ

2000 nM (IC₅₀)

体外研究
(In Vitro)

GW9662 inhibits radioligand binding to PPARγ, PPARα, and PPARδ with pIC₅₀s of 8.48±0.27 (IC₅₀=3.3 nM; n=10), 7.49±0.17 (IC₅₀=32 nM; n=9), and 5.69±0.17 (IC₅₀=2000 nM; n=3), respectively. GW9662 has nanomolar IC₅₀ versus PPARγ and is 10- and 600-fold less potent in binding experiments using PPARα and PPARδ, respectively. In cell-based reporter assays, GW9662 is a potent and selective antagonist of full-length PPARγ^[1]. Co-treatment with both 50 μM BRL 49653 and 10 μM GW9662 results in statistically lower viable cell numbers after 7 days when compared to treatment with either 50 μM BRL 49653 (P=0.001) or 10 μM GW9662 (P=0.01) alone^[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

Bone marrow (BM) nucleated cell counts in both BADGE- and GW9662(1 mg/kg, i.p.)-treated mice are significantly higher than counts in the aplastic anemia (AA) group^[3]. GW9662 (1 mg/kg, i.p.) largely attenuates the renoprotective effects of Lipopolysaccharide (LPS) in the rat^[4].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

276.68

Formula

C₁₃H₉ClN₂O₃

CAS 号

22978-25-2

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

In Vitro:

DMSO : ≥ 100 mg/mL (361.43 mM)

* “≥” means soluble, but saturation unknown.

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	3.6143 mL	18.0714 mL	36.1428 mL
5 mM	0.7229 mL	3.6143 mL	7.2286 mL
10 mM	0.3614 mL	1.8071 mL	3.6143 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline

Solubility: ≥ 2.5 mg/mL (9.04 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (9.04 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% corn oil

Solubility: ≥ 2.5 mg/mL (9.04 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (9.04 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。
3.

请依序添加每种溶剂： 1% DMSO 99% saline

Solubility: ≥ 0.5 mg/mL (1.81 mM); Clear solution

*以上所有助溶剂都可在上海金畔生物科技有限公司网站选购。

参考文献

[1]. Leesnitzer LM, et al. Functional consequences of cysteine modification in the ligand binding sites of peroxisome proliferator activated receptors by GW9662. Biochemistry. 2002 May 28;41(21):6640-50.

[2]. Seargent JM, et al. GW9662, a potent antagonist of PPARgamma, inhibits growth of breast tumor cells and promotes the anticancer effects of the PPARgamma agonist BRL 49653, independently of PPARgamma activation. Br J Pharmacol. 2004 Dec;143(8):933-7.

[3]. Sato K, et al. PPARγ antagonist attenuates mouse immune-mediated bone marrow failure by inhibition of T cell function.Haematologica. 2016 Jan;101(1):57-67.

[4]. Collino M, et al. The selective PPARgamma antagonist GW9662 reverses the protection of LPS in a model of renal ischemia-reperfusion. Kidney Int. 2005 Aug;68(2):529-36.

Cell Assay ^[2]	Cells (MCF7, MDA-MB-231, MDA-MB-468) are plated in 96-well plates at a density of 1×10³ cells per well in RPMI medium. After overnight incubation to allow for cell attachment, the medium is removed and replaced with fresh medium containing varying concentrations of BRL 49653 (1-100 μM), GW9662 (100 nM-50 μM) or solvent (DMSO) alone. MDA-MB-231 cells are also subjected to combinations of BRL 49653 (10, 50 μM) and GW9662 (1, 10 μM) added simultaneously. The final concentration of DMSO in all cases does not exceed 0.1% and is not found to be cytotoxic in any of the cell lines tested at this concentration. Chemosensitivity is assessed following a continuous 72 h exposure using a standard MTT assay. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[3]^[4]	Mice^[3] Inbred C57BL/6 (B6, H2^b/b), DBA/1J (DBA/1, H2^q/q), FVB/NJ (FVB, H2^q/q) mice and congenic C.B10-H2^b/b/LilMcd (CB10, H2^b/b) mice are used. BADGE or GW9662, are administrated by daily intraperitoneal injection at 30 mg/kg for BADGE, or at 1 mg/kg for GW9662, from one day prior to the experiment and continued for up to 2 weeks. In the FVB AA model, some mice are injected with CsA (50 mg/kg/day) starting 1 hour after the LN injection, and continued for 5 days as immunosuppression. At the end of the experiments, the mice are euthanized by CO₂ inhalation. Rats^[4] Sixty-two male Wistar rats weighing 215 to 315 g are used in this study. Animals are randomly allocated into 6 groups as follows: (1) I/R group: control, rats are administered 10% (v/v) DMSO (vehicle for GW9662, 1 mL /kg, IP) 24 and 12 hours prior to renal I/R, and saline (vehicle for LPS, 1 mL /kg, IP) 24 hours prior to renal I/R (N=12); (2) I/R LPS group: rats are administered 10% (v/v) DMSO (vehicle for GW9662, 1 mL /kg, IP) 24 and 12 hours prior to renal I/R, and LPS (1 mg/kg, IP) 24 hours prior to renal I/R (N=11); (3) I/R GW9662 group: rats are administered GW9662 (1 mg/kg, IP) 24 and 12 hours prior to renal I/R, and saline (vehicle for LPS, 1 mL /kg, IP) 24 hours prior to renal I/R (N=9); (4) I/R LPS+GW9662 group: rats are administered GW9662 (1 mg/kg, IP) 24 and 12 hours prior to renal I/R, and LPS (1 mg/kg, IP) 24 hours prior to renal I/R (N=11); (5) Sham group: rats are subjected to the same surgical procedures as above, except for renal I/R. Rats are administered 10% (v/v) DMSO (vehicle for GW9662, 1 mL /kg, IP) and saline (vehicle for LPS, 1 mL /kg, IP) at times equivalent to those described above (N=12); (6) Sham GW9662 group: rats are subjected to the same surgical procedures as above, except for renal I/R. Rats are administered GW9662 (1 mg/kg, IP) and saline (vehicle for LPS, 1 mL /kg, IP) at times equivalent to those described above (N=7). 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献	[1]. Leesnitzer LM, et al. Functional consequences of cysteine modification in the ligand binding sites of peroxisome proliferator activated receptors by GW9662. Biochemistry. 2002 May 28;41(21):6640-50. [2]. Seargent JM, et al. GW9662, a potent antagonist of PPARgamma, inhibits growth of breast tumor cells and promotes the anticancer effects of the PPARgamma agonist BRL 49653, independently of PPARgamma activation. Br J Pharmacol. 2004 Dec;143(8):933-7. [3]. Sato K, et al. PPARγ antagonist attenuates mouse immune-mediated bone marrow failure by inhibition of T cell function.Haematologica. 2016 Jan;101(1):57-67. [4]. Collino M, et al. The selective PPARgamma antagonist GW9662 reverses the protection of LPS in a model of renal ischemia-reperfusion. Kidney Int. 2005 Aug;68(2):529-36.

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GW 4064

发表于2024年10月23日由上海金畔生物科技有限公司

GW 4064 纯度: 99.76%

GW 4064 是一种有效的 FXR 激动剂，EC₅₀ 为 65 nM。

GW 4064 Chemical Structure

CAS No. : 278779-30-9

规格	价格	是否有货
Free Sample (0.1-0.5 mg)		Apply now
10 mM * 1 mL in DMSO	￥615	In-stock
5 mg	￥515	In-stock
10 mg	￥818	In-stock
50 mg	￥2727	In-stock
100 mg	￥4990	In-stock
200 mg	￥8500	In-stock
500 mg		询价
1 g		询价

* Please select Quantity before adding items.

GW 4064 相关产品

•相关化合物库:

Bioactive Compound Library Plus
Metabolism/Protease Compound Library
Anti-Cancer Compound Library
Autophagy Compound Library

生物活性

GW 4064 is a potent FXR agonist with an EC₅₀ of 65 nM.

IC₅₀ & Target

EC50: 65 nM (FXR)^[1]

体外研究
(In Vitro)

Treatment with different concentrations of GW4064 (1, 2.5, 5, 10 μM) reduces the lipid accumulation in the cells. Concordantly, GW4064 treatment significantly represses oleic acid-induced CD36 protein levels in a dose-dependent manner. Taken together, these data indicate that prevention of hepatic lipid accumulation is likely due to an inhibition of Cd36 expression by long-term GW4064 treatment^[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

GW4064 suppresses weight gain in C57BL/6 mice fed with either a high-fat diet (HFD) or high-fat, high-cholesterol diet. GW4064 treatment of mice on HFD significantly represses diet-induced hepatic steatosis as evidenced by lower triglyceride and free fatty acid level in the liver. GW4064 markedly reduces lipid transporter CD36 expression without affecting expression of genes that are directly involved in lipogenesis. GW4064 treatment attenuates hepatic inflammation while having no effect on white adipose tissue^[2]. GW4064 (30 mg/kg) treatment results in substantial, statistically significant reductions in serum activities of ALT, AST, LDH, and ALP in the ANIT-treated rats. Serum bile acid levels are also significantly reduced by GW4064 treatment. Bilirubin levels are decreased in the GW4064-treated rats, but statistical significance is not achieved. Notably, GW4064 is much more effective in decreasing these markers of liver damage than TUDCA, which reduces only LDH levels^[3].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

542.84

Formula

C₂₈H₂₂Cl₃NO₄

CAS 号

278779-30-9

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

In Vitro:

DMSO : 125 mg/mL (230.27 mM; Need ultrasonic)

DMF : 100 mg/mL (184.22 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.8422 mL	9.2108 mL	18.4216 mL
5 mM	0.3684 mL	1.8422 mL	3.6843 mL
10 mM	0.1842 mL	0.9211 mL	1.8422 mL

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

1.

请依序添加每种溶剂： 10% DMF 40% PEG300 5% Tween-80 45% saline

Solubility: ≥ 2.5 mg/mL (4.61 mM); Clear solution
2.

请依序添加每种溶剂： 10% DMF 90% corn oil

Solubility: ≥ 2.5 mg/mL (4.61 mM); Clear solution
3.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline

Solubility: ≥ 2.5 mg/mL (4.61 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (4.61 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
4.

请依序添加每种溶剂： 10% DMSO 90% corn oil

Solubility: ≥ 2.08 mg/mL (3.83 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (3.83 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在上海金畔生物科技有限公司网站选购。

参考文献

[1]. Akwabi-Ameyaw A, et al.Conformationally constrained farnesoid X receptor (FXR) agonists: Naphthoic acid-based analogs of GW 4064. Bioorg Med Chem Lett, 2008, 18(15), 4339-4343.

[2]. Ma Y, et al. Synthetic FXR agonist GW4064 prevents diet-induced hepatic steatosis and resistance. Pharm Res. 2013 May;30(5):1447-57.

[3]. Liu Y, et al. Hepatoprotection by the farnesoid X receptor agonist GW4064 in rat models of intra- and extrahepatic cholestasis. J Clin Invest. 2003 Dec;112(11):1678-87.

Cell Assay ^[2]	Mouse liver cells (BNL CL.2) are maintained in a humidified incubator under 5% CO2 at 37°C in Dulbecco’s Modified Eagle’s Medium (DMEM). When cells are divided into six-well plates and reach ~90% confluence, sub-confluent cells are washed three times with phosphate buffered saline (PBS) and replaced with serum-free DMEM supplemented with 1% fatty acid-free BSA. Oleic acid (final concentration 500 μM) and GW4064 at various concentrations are added and incubated for 24 h. Cells are then fixed with 4% formaldehyde for Oil Red O staining or harvested for protein and western blot analysis^[2]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[2]^[3]	Mice^[2] Fifteen-week-old male C57BL/6 mice are fed a high-fat diet with or without additional 0.2% Cholesterol and received twice weekly injections of GW 4064 (50 mg/kg, intra-peritoneal) or carrier solution (DMSO) solution for 6 weeks. Animals are weighed weekly and their body composition is determined using EchoMRI-100^TM from Echo Medical Systems. Rats^[3] Animals. Adult male CRL:CD(SD)IGS rats weighing 300-350 g, are used. Twenty-four hours after laparotomy, groups of rats (n=6) receive intraperitoneal injections once daily for 4 days. Bile duct-ligated (BDL) rats are treated with 5 mL/kg corn oil as vehicle, 30 mg/kg GW4064 in corn oil, or 15 mg/kg TUDCA in corn oil. Sham-operated animals received 5 mL/kg corn oil vehicle. Four hours after the final dose, serum and livers are collected for analysis. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献	[1]. Akwabi-Ameyaw A, et al.Conformationally constrained farnesoid X receptor (FXR) agonists: Naphthoic acid-based analogs of GW 4064. Bioorg Med Chem Lett, 2008, 18(15), 4339-4343. [2]. Ma Y, et al. Synthetic FXR agonist GW4064 prevents diet-induced hepatic steatosis and resistance. Pharm Res. 2013 May;30(5):1447-57. [3]. Liu Y, et al. Hepatoprotection by the farnesoid X receptor agonist GW4064 in rat models of intra- and extrahepatic cholestasis. J Clin Invest. 2003 Dec;112(11):1678-87.

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Lapatinib(Synonyms: 拉帕替尼; GW572016; GW2016)

发表于2024年10月22日由上海金畔生物科技有限公司

Lapatinib (Synonyms: 拉帕替尼; GW572016; GW2016) 纯度: 99.83%

Lapatinib (GW572016) 是一种 ErbB-2 和 EGFR 酪氨酸激酶结构域的有效抑制剂，对纯化的 EGFR 和 ErbB-2 的 IC₅₀ 值分别为 10.2 和 9.8 nM。

Lapatinib Chemical Structure

CAS No. : 231277-92-2

规格	价格	是否有货
Free Sample (0.1-0.5 mg)		Apply now
10 mM * 1 mL in DMSO	￥770	In-stock
50 mg	￥700	In-stock
100 mg	￥1200	In-stock
500 mg	￥3000	In-stock
1 g	￥4500	In-stock
5 g		询价
10 g		询价

* Please select Quantity before adding items.

Lapatinib 相关产品

•相关化合物库:

Covalent Screening Library Plus
Drug Repurposing Compound Library Plus
FDA-Approved Drug Library Plus
FDA-Approved Drug Library Mini
Bioactive Compound Library Plus
Apoptosis Compound Library
Immunology/Inflammation Compound Library
JAK/STAT Compound Library
Kinase Inhibitor Library
Protein Tyrosine Kinase Compound Library
FDA-Approved Drug Library
Anti-Cancer Compound Library
CNS-Penetrant Compound Library
Autophagy Compound Library
Drug Repurposing Compound Library
Covalent Screening Library
Differentiation Inducing Compound Library
Ferroptosis Compound Library
Anti-COVID-19 Compound Library
Orally Active Compound Library
FDA Approved & Pharmacopeial Drug Library
Anti-Hepatitis C Virus Compound Library
Anti-Breast Cancer Compound Library
Anti-Lung Cancer Compound Library
Drug-Induced Liver Injury (DILI) Compound Library
Anti-Pancreatic Cancer Compound Library
Targeted Therapy Drug Library
Angiogenesis Related Compound Library
Anti-Liver Cancer Compound Library
Rare Diseases Drug Library
Anti-Colorectal Cancer Compound Library

生物活性

Lapatinib (GW572016) is a potent inhibitor of the ErbB-2 and EGFR tyrosine kinase domains with IC₅₀ values against purified EGFR and ErbB-2 of 10.2 and 9.8 nM, respectively^[1].

IC₅₀ & Target

EGFR

10.2 nM (IC₅₀, Cell Free Assay)

ErbB2

9.8 nM (IC₅₀, Cell Free Assay)

体外研究
(In Vitro)

Lapatinib (GW2016; 0.03-10 µM; 6 hours; BT474 and HN5 cells) treatment inhibits receptor autophosphorylation of EGFR and ErbB-2 in a dose-responsive manner. Phosphorylation of serine 473 of AKT was inhibited by GW2016 in a dose-dependent manner^[1].
Lapatinib (GW2016; 72 hours; HN5, A-43, BT474, N87, and CaLu-3 cells) treatment has a selective inhibition of the proliferation of human tumor cell lines^[1].
Lapatinib (GW2016; 1-10 µM; 72 hours; HN5 cells) treatment results in induces G1 arrest^[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis^[1]

Cell Line:	BT474 and HN5 cells
Concentration:	0.03 µM, 0.1 µM, 0.3 µM, 1 µM, 3 µM, or 10 µM
Incubation Time:	6 hours
Result:	Inhibited receptor autophosphorylation of EGFR and ErbB-2 in a dose-responsive manner. Phosphorylation of serine 473 of AKT was also inhibited in a dose-dependent manner.

Cell Proliferation Assay^[1]

Cell Line:	HN5, A-43, BT474, N87, and CaLu-3 cells
Concentration:
Incubation Time:	72 hours
Result:	Inhibited the growth of tumor cells overexpressing EGFR or ErbB-2.

Cell Cycle Analysis^[1]

Cell Line:	HN5 cells
Concentration:	1 µM, or 10 µM
Incubation Time:	72 hours
Result:	Resulted in induction of G1 arrest.

体内研究
(In Vivo)

Lapatinib (GW2016; 30-100 mg/kg; oral administration; twice daily; for 21 days; CD-1 nude female mice) treatment inhibits tumor xenograft growth of the HN5 cells in a dose-responsive manner at 30 and 100 mg/kg, with complete inhibition of tumor growth at the higher dose^[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	CD-1 nude female mice (4-6 weeks old) with HN5 cells^[1]
Dosage:	30 mg/kg, 100 mg/kg
Administration:	Oral administration; twice daily; for 21 days
Result:	Inhibited tumor xenograft growth of the HN5 cells in a dose-responsive manner.

Clinical Trial

分子量

581.06

Formula

C₂₉H₂₆ClFN₄O₄S

CAS 号

231277-92-2

中文名称

拉帕替尼

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

In Vitro:

DMSO : 125 mg/mL (215.12 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.7210 mL	8.6050 mL	17.2099 mL
5 mM	0.3442 mL	1.7210 mL	3.4420 mL
10 mM	0.1721 mL	0.8605 mL	1.7210 mL

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

1.

请依序添加每种溶剂： 12% SBE-beta-CD

Solubility: 5 mg/mL (8.60 mM); Suspended solution; Need ultrasonic
2.

请依序添加每种溶剂： 5% DMSO 95% (20% SBE-β-CD in saline)

Solubility: 2.5 mg/mL (4.30 mM); Suspended solution; Need ultrasonic
3.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline

Solubility: ≥ 2.08 mg/mL (3.58 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (3.58 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
4.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)

Solubility: 2.08 mg/mL (3.58 mM); Suspended solution; Need ultrasonic

此方案可获得 2.08 mg/mL (3.58 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。

以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
5.

请依序添加每种溶剂： 10% DMSO 90% corn oil

Solubility: ≥ 2.08 mg/mL (3.58 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (3.58 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在 MCE 网站选购。

参考文献

[1]. Rusnak DW, et al. The effects of the novel, reversible epidermal growth factor receptor/ErbB-2 tyrosine kinase inhibitor, GW2016, on the growth of human normal and tumor-derived cell lines in vitro and in vivo. Mol Cancer Ther. 2001 Dec;1(2):85-94

GW6471

发表于2024年10月17日由上海金畔生物科技有限公司

GW6471 纯度: 98.71%

GW6471 是一种有效的 PPARα 拮抗剂。

GW6471 Chemical Structure

CAS No. : 880635-03-0

规格	价格	是否有货
10 mM * 1 mL in DMSO	￥2181	In-stock
5 mg	￥1600	In-stock
10 mg	￥2500	In-stock
50 mg	￥9400	In-stock
100 mg		询价

* Please select Quantity before adding items.

GW6471 相关产品

•相关化合物库:

Bioactive Compound Library Plus
Cell Cycle/DNA Damage Compound Library
Anti-Cancer Compound Library
Anti-Aging Compound Library
Transcription Factor Targeted Library
Lipid Metabolism Compound Library

生物活性

GW6471 is a potent PPARα antagonist.

IC₅₀ & Target^[1]

PPARα

体外研究
(In Vitro)

In a cell-based reporter assay, GW6471 completely inhibits GW409544-induced activation of PPARα with an IC₅₀ of 0.24 μM^[1]. The functional role of PPARα is evaluated on renal cell carcinoma (RCC) cell viability by MTT assay. Both Caki-1 (VHL wild type) and 786-O (VHL mutated) cells are incubated separately with a specific PPARα agonist, WY14,643, or a specific PPARα antagonist, GW6471 at concentrations from 12.5 to 100 µM for 72 hours, and cell viability is assessed. While WY14,643 either has no affect on, or slightly increased, cell viability, GW6471 significantly and dose-dependently inhibits cell viability (up to approximately 80%) in both cell lines^[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

To test the antitumor activity of PPARα antagonism in vivo, a subcutaneous xenograft mouse model is used. Caki-1 cells are implanted subcutaneously in nude (Nu/Nu) mice. After tumor masses reach ∼5 mm in diameter, GW6471 is administrated intraperitoneally every other day for 4 wk at a dose (20 mg/kg mouse body wt) that is described to be effective in an in vivo dose-response study and confirmed here to be efficacious. There are significant differences in tumor growth between vehicle- and GW6471-treated animals. No toxicity is observed at the doses of GW6471 based on weights of the animals, and laboratory values, including kidney and liver function tests, are not adversely affected. To demonstrate on-target effects of GW6471, c-Myc levels are evaluated in the tumors, which show significant decreases in the GW6471-treated animals^[3].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

619.67

Formula

C₃₅H₃₆F₃N₃O₄

CAS 号

880635-03-0

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

In Vitro:

DMSO : 125 mg/mL (201.72 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.6138 mL	8.0688 mL	16.1376 mL
5 mM	0.3228 mL	1.6138 mL	3.2275 mL
10 mM	0.1614 mL	0.8069 mL	1.6138 mL

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline

Solubility: ≥ 2.08 mg/mL (3.36 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (3.36 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)

Solubility: 2.08 mg/mL (3.36 mM); Suspended solution; Need ultrasonic

此方案可获得 2.08 mg/mL (3.36 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。

以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil

Solubility: ≥ 2.08 mg/mL (3.36 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (3.36 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在上海金畔生物科技有限公司网站选购。

参考文献

[1]. Xu HE, et al. Structural basis for antagonist-mediated recruitment of nuclear co-repressors by PPARalpha. Nature. 2002 Feb 14;415(6873):813-7.

[2]. Abu Aboud O, et al. Inhibition of PPARα induces cell cycle arrest and apoptosis, and synergizes with glycolysisinhibition in kidney cancer cells. PLoS One. 2013 Aug 7;8(8):e71115.

[3]. Abu Aboud O, et al. PPARα inhibition modulates multiple reprogrammed metabolic pathways in kidney cancer and attenuates tumor growth. Am J Physiol Cell Physiol. 2015 Jun 1;308(11):C890-8.

Cell Assay ^[2]	786-O and Caki-1 cells are plated in 96 well plates. Both cells are incubated separately with WY14,643 or GW 6471 at concentrations from 12.5 to 100 µM for 72 hours, and after the indicated treatments, the cells are incubated in MTT solution/media mixture. Then, the MTT solution is removed and the blue crystalline precipitate in each well is dissolved in DMSO. Visible absorbance of each well at 540 nm is quantified using a microplate reader^[2]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[3]	Mice^[3] *Male athymic Nu/Nu* mice (8 wk of age, ~25 g body wt) are injected with 1×10⁵ Caki-1 cells subcutaneously (3:1 DMEM-Matrigel) in the flank region. Tumor progression is monitored weekly by calipers. When tumor size reaches ~80-100 mm³, animals are randomly assigned to four groups and treatments are started (day 1). The vehicle group receive DMSO (4% in PBS) intraperitoneally and vegetable oil via oral gavage. The PPARα group is injected intraperitoneally with GW 6471 in the same vehicle (20 mg/kg body wt; murine dose response is reported elsewhere) every other day. The Sunitinib group receive Sunitinib in vegetable oil via oral gavage (40 mg/kg body wt) 5 days/wk. Another group receive GW 6471+Sunitinib. To determine any potential toxicity of the treatment(s), body weights of the animals are measured and signs of adverse reactions are monitored. On day 28, the mice are euthanized and the tumor mass is determined. Tumor growth rate is calculated^[3]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.**
参考文献	[1]. Xu HE, et al. Structural basis for antagonist-mediated recruitment of nuclear co-repressors by PPARalpha. Nature. 2002 Feb 14;415(6873):813-7. [2]. Abu Aboud O, et al. Inhibition of PPARα induces cell cycle arrest and apoptosis, and synergizes with glycolysisinhibition in kidney cancer cells. PLoS One. 2013 Aug 7;8(8):e71115. [3]. Abu Aboud O, et al. PPARα inhibition modulates multiple reprogrammed metabolic pathways in kidney cancer and attenuates tumor growth. Am J Physiol Cell Physiol. 2015 Jun 1;308(11):C890-8.

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Pazopanib(Synonyms: 帕唑帕尼; GW786034)

发表于2024年10月17日由上海金畔生物科技有限公司

Pazopanib (Synonyms: 帕唑帕尼; GW786034) 纯度: 99.77%

Pazopanib (GW786034) 是多靶点抑制剂，抑制 VEGFR1，VEGFR2，VEGFR3，PDGFRβ，c-Kit，FGFR1，c-Fms的IC₅₀分别为10，30，47，84，74，140，146 nM。

Pazopanib Chemical Structure

CAS No. : 444731-52-6

规格	价格	是否有货
Free Sample (0.1-0.5 mg)		Apply now
10 mM * 1 mL in DMSO	￥572	In-stock
10 mg	￥520	In-stock
50 mg	￥1100	In-stock
100 mg	￥1600	In-stock
200 mg	￥2700	In-stock
500 mg	￥4500	In-stock
1 g		询价
5 g		询价

* Please select Quantity before adding items.

Pazopanib 相关产品

•相关化合物库:

Drug Repurposing Compound Library Plus
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Drug-Induced Liver Injury (DILI) Compound Library
Anti-Pancreatic Cancer Compound Library
Anti-Blood Cancer Compound Library
Targeted Therapy Drug Library
Angiogenesis Related Compound Library
Anti-Liver Cancer Compound Library
Rare Diseases Drug Library
Anti-Colorectal Cancer Compound Library

生物活性

Pazopanib (GW786034) is a novel multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFRβ, c-Kit, FGFR1, and c-Fms with IC₅₀s of 10, 30, 47, 84, 74, 140 and 146 nM, respectively.

IC₅₀ & Target^[1]

VEGFR1

10 nM (IC₅₀)

VEGFR2

30 nM (IC₅₀)

VEGFR3

47 nM (IC₅₀)

PDGFRβ

84 nM (IC₅₀)

FGFR1

140 nM (IC₅₀)

c-Kit

74 nM (IC₅₀)

c-Fms

146 nM (IC₅₀)

体外研究
(In Vitro)

Pazopanib shows good potency against all the human VEGFR receptors with an IC₅₀ of 10, 30, and 47 nM for VEGFR-1, -2, and -3, respectively. Significant activity is also seen against the closely related tyrosine receptor kinases PDGFRβ, c-Kit, FGF-R1, and c-fms with IC₅₀s of 84, 74, 140, and 146 nM, respectively. In cellular assays, in addition to inhibiting the VEGF-induced proliferation of HUVECs, Pazopanib potently inhibits VEGF-induced phosphorylation of VEGFR-2 in HUVEC cells with an IC₅₀ of ~8 nM. Pazopanib possesses good pharmacokinetics in rat, dog, and monkey with low clearances (1.4-1.7 mL/min/kg) and good oral bioavailabilities (72, 47, 65%) dosed at 10, 1, and 5 mg/kg, respectively. The cytochrome P450 profile is also improved with inhibition >10 μM against the isozymes tested, with the exception of 2C9 (7.9 μM)^[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

Treatment of mice with 100 mg/kg of Pazopanib twice daily for five days results in significant inhibition in the degree of vascularization. The antiangiogenic activity of Pazopanib is examined in mice bearing established human xenografts (200−250 mm³) using HT29 (colon carcinoma), A375P (melanoma), and HN5 (head and neck carcinoma) tumors following a standard three-week course of therapy. The HN5 and HT29 xenografts responded better at all doses compared to the A375P model, which is historically more resistant to VEGFR-2 inhibitors. As support that the observed inhibition of xenograft growth is working through an antiangiogenic rather than antitumor mechanism, no antiproliferative activity is observed below 10 μM for Pazopanib against these human tumor lines (HT29, HN5, A375P) growing in serum-containing media. No significant effect on the body weight of mice is observed, and the animals appeared healthy and active throughout the study duration^[1]. The quantity of adherent leukocytes in the Pazopanib eye drops group is less than untreated diabetic animals and more than the healthy animals. Average leukocytes adhered to the retinal vasculature in healthy animals is 37.2±7.8, whereas diabetic animals have an average value of 102±15.6, approximately 3-fold higher than healthy animals. Animals treated with 0.5 % w/v Pazopanib suspension demonstrate 69.5±9.5 leukocytes adhered in their retinal vasculature, which is found to be significantly lower than diabetic animals^[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

分子量

437.52

Formula

C₂₁H₂₃N₇O₂S

CAS 号

444731-52-6

中文名称

帕唑帕尼

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

In Vitro:

DMSO : 62.5 mg/mL (142.85 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.2856 mL	11.4280 mL	22.8561 mL
5 mM	0.4571 mL	2.2856 mL	4.5712 mL
10 mM	0.2286 mL	1.1428 mL	2.2856 mL

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

1.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)

Solubility: ≥ 2.5 mg/mL (5.71 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (5.71 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
2.

请依序添加每种溶剂： 10% DMSO 90% corn oil

Solubility: ≥ 2.5 mg/mL (5.71 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (5.71 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。
3.

请依序添加每种溶剂： 5% DMSO 40% PEG300 5% Tween-80 50% saline

Solubility: ≥ 0.43 mg/mL (0.98 mM); Clear solution
4.

请依序添加每种溶剂： 5% DMSO 95% (20% SBE-β-CD in saline)

Solubility: ≥ 0.43 mg/mL (0.98 mM); Clear solution

*以上所有助溶剂都可在上海金畔生物科技有限公司网站选购。

参考文献

[1]. Harris PA, et al. Discovery of 5-[[4-[(2,3-dimethyl-2H-indazol-6-yl)methylamino]-2-pyrimidinyl]amino]-2-methyl-benzenesulfonamide (Pazopanib), a novel and potent vascular endothelial growth factor receptor inhibitor. J Med Chem. 2008, 51(15), 4632-4640.

[2]. Thakur A, et al. Pazopanib, a multitargeted tyrosine kinase inhibitor, reduces diabetic retinal vascular leukostasis and leakage. Microvasc Res. 2011 Nov;82(3):346-50.

Kinase Assay ^[1]	VEGFR enzyme assays for VEGGR1, VEGFR2, and VEGFR3 are run in homogeneous time-resolved fluorescence (HTRF) format in 384-well microtiter plates using a purified, baculovirus-expressed glutathione-S-transferase (GST) fusion protein encoding the catalytic c-terminus of human VEGFR receptor kinases 1, 2, or 3. Reactions are initiated by the addition of 10 μL of activated VEGFR2 kinase solution [final concentration, 1 nM enzyme in 0.1 M 4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid (HEPES), pH 7.5, containing 0.1 mg/mL bovine serum albumin (BSA), 300 μM dithiothreitol (DTT)] to 10 μL substrate solution [final concentration, 360 nM peptide, (biotin-aminohexyl-EEEEYFELVAKKKK-NH2), 75 μM ATP, 10 μM MgCl₂], and 1 μL of titrated compound in DMSO. Plates are incubated at room temperature for 60 min, and then the reaction is quenched by the addition of 20 μL of 100 mM ethylene diamine tetraacetic acid (EDTA). After quenching, 20 μL HTRF reagents (final concentration, 15 nM Streptavidin-linked allophycocyanin, 1 nM Europium-labeled antiphosphotyrosine antibody diluted in 0.1 mg/mL BSA, 0.1 M HEPES, pH 7.5) is added and the plates incubated for a minimum of 10 min. The fluorescence at 665 nM is measured with a Wallac Victor plate reader using a time delay of 50 μs^[1]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Assay ^[1]	The effect of Pazopanib on cell proliferation is measured using 5-bromo-2-deoxyuridine (BrdU) incorporation method using commercially available kits. HUVEC is seeded in medium containing 5% fetal bovine serum (FBS) in type 1 collagen coated 96-well plates and incubated overnight at 37°C, 5% CO₂. The medium is aspirated from the cells, and various concentrations of Pazopanib in serum-free medium are added to each well. After 30 min, either VEGF (10 ng/mL) or bFGF (0.3 ng/mL) is added to the wells. Cells are incubated for an additional 72 h and BrdU (10 μM) is added during the last 18 to 24 h of incubation. At the end of incubation, BrdU incorporation in cells is measured by ELISA. Data are fitted with a curve described by the equation, y=V_max(1−(x/(K+x))), where K is equal to the IC₅₀^[1]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[1]^[2]	Mice^[1] Tumors are initiated by injection of tumor cell suspension in 8−12 week old nude mice. When tumors reach a volume of 100−200 mm³, mice are randomized and divided into groups of eight. Pazopanib is administered once or twice daily at 10, 30, or 100 mg/kg. Animals are euthanized by inhalation of CO₂ at the completion of the study. Tumor volume is measured twice weekly by calipers, using the equation: tumor volume (mm³)=(length×width²)/2. Results are routinely reported as % inhibition=1−(average growth of the drug treated population/average growth of vehicle treated control population). Rats^[2] Male Brown-Norway (BN; pigmented) rats weighing 200 to 250 g are acclimatized for at least two days prior to any experimental procedure. After overnight fasting for 12-16 h, an intraperitoneal injection of 30 mg/mL solution of Streptozotocin in 10 mM citrate buffer (pH 4.5) is administered (60 mg/kg body weight) to induce diabetes. After 3-4 h of Streptozotocin injection, animals are put on a regular diet and 24 h after Streptozotocin injection, blood sample (5-10 μL) is collected via tail vein. The blood glucose levels in the animals are determined with a glucose monitor. Animals with blood glucose levels greater than 250 mg/dL are considered diabetic. The animals are divided into three groups. Group 1: Healthy (n=12), Group 2: Diabetic (n=12) and Group 3: Diabetic+Treatment (n=12). Treatment is started immediately after diabetes induction. Both eyes are dosed twice daily for 30 days with 0.5 % w/v Pazopanib suspension (10 μL volume in each eye) and animals in all groups are sacrificed on day 31, 16-17 h after last dose on day 30. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献	[1]. Harris PA, et al. Discovery of 5-[[4-[(2,3-dimethyl-2H-indazol-6-yl)methylamino]-2-pyrimidinyl]amino]-2-methyl-benzenesulfonamide (Pazopanib), a novel and potent vascular endothelial growth factor receptor inhibitor. J Med Chem. 2008, 51(15), 4632-4640. [2]. Thakur A, et al. Pazopanib, a multitargeted tyrosine kinase inhibitor, reduces diabetic retinal vascular leukostasis and leakage. Microvasc Res. 2011 Nov;82(3):346-50.

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GW627368

发表于2024年10月12日由上海金畔生物科技有限公司

GW627368 纯度: 99.97%

GW627368 (GW627368X) 是前列腺素受体 EP4 高效选择竞争性抑制剂，还对血栓素受体 TP 有亲和力。对人 EP4 和 TP 的 pK_i 值分别为 7.0 和 6.8。

GW627368 Chemical Structure

CAS No. : 439288-66-1

规格	价格	是否有货
Free Sample (0.1-0.5 mg)		Apply now
10 mM * 1 mL in DMSO	￥1438	In-stock
5 mg	￥1200	In-stock
10 mg	￥2050	In-stock
25 mg	￥4100	In-stock
50 mg	￥6950	In-stock
100 mg	￥11850	In-stock
200 mg		询价
500 mg		询价

* Please select Quantity before adding items.

GW627368 相关产品

•相关化合物库:

Bioactive Compound Library Plus
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生物活性

GW627368 (GW627368X) is a novel, potent and selective competitive antagonist of prostanoid EP4 receptor with additional human TP receptor affinity, with pK_i values of 7.0 and 6.8 for human prostanoid EP4 and TP receptors respectively^[1].

IC₅₀ & Target

pKi ：7.0 (hEP4), 6.8 (hTP)^[1]

体外研究
(In Vitro)

GW627368 (GW627368X) appears to bind to human prostanoid TP receptors but not the TP receptors of other species^[1].
GW627368 (GW627368X) (10 μM) produces 100% inhibition of U-46619 (EC₁₀₀)-induced aggregation (approximate pA2 approximately 7.0) in human washed platelets^[1].
GW627368 (GW627368X) is devoid of agonist activity and actually produced a significant and concentration-related reduction in basal cAMP levels with pIC₅₀ value of 6.3^[1].
GW627368 (GW627368X) induces inhibition of proliferation and invasion of human SUM149 IBC tumor cells beginning at 0.1 μM, with inhibition of proliferation and invasion of MDA-MB-231 non-IBC cells at higher concentrations^[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

GW627368 (GW627368X) (0-15 mg/kg; p.o.; every alternate day for 28 days) shows significant tumor regression characterized by tumor reduction and induction of apoptosis^[3].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	6-8 weeks Swiss albino mice^[3]
Dosage:	0 mg/kg, 5 mg/kg, 10 mg/kg, 15 mg/kg, 15 mg/kg
Administration:	Oral administration, every alternate day for 28 days
Result:	Displayed anti-tumor and anti-proliferative potential in sarcoma 180 bearing mice.

分子量

544.62

Formula

C₃₀H₂₈N₂O₆S

CAS 号

439288-66-1

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

In Vitro:

DMSO : 100 mg/mL (183.61 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.8361 mL	9.1807 mL	18.3614 mL
5 mM	0.3672 mL	1.8361 mL	3.6723 mL
10 mM	0.1836 mL	0.9181 mL	1.8361 mL

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline

Solubility: ≥ 2.5 mg/mL (4.59 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (4.59 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% corn oil

Solubility: ≥ 2.5 mg/mL (4.59 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (4.59 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在上海金畔生物科技有限公司网站选购。

参考文献

[1]. Wilson RJ, et al. GW627368X ((N-{2-[4-(4,9-diethoxy-1-oxo-1,3-dihydro-2H-benzo[f]isoindol-2-yl)phenyl]acetyl} benzene sulphonamide): a novel, potent and selective prostanoid EP4 receptor antagonist. Br J Pharmacol. 2006 Jun;148(3):326-39.

[2]. Robertson FM, et al. Molecular and pharmacological blockade of the EP4 receptor selectively inhibits both proliferation and invasion of human inflammatory breast cancer cells. J Exp Ther Oncol. 2008;7(4):299-312.

[3]. Parida S, et al. Molecular inhibition of prostaglandin E2 with GW627368X: Therapeutic potential and preclinical safety assessment in mouse sarcoma model. Cancer Biol Ther. 2015;16(6):922-32.

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GW3965 hydrochloride

发表于2024年10月11日由上海金畔生物科技有限公司

GW3965 hydrochloride 纯度: 99.73%

GW3965 hydrochloride 是肝 X 受体 (LXR) 激动剂，对 hLXRα 和 hLXRβ 的 EC₅₀ 分别为 190 nM 和 30 nM。

GW3965 hydrochloride Chemical Structure

CAS No. : 405911-17-3

规格	价格	是否有货
Free Sample (0.1-0.5 mg)		Apply now
10 mM * 1 mL in DMSO	￥953	In-stock
5 mg	￥700	In-stock
10 mg	￥1000	In-stock
50 mg	￥3900	In-stock
100 mg	￥7400	In-stock
200 mg		询价
500 mg		询价

* Please select Quantity before adding items.

GW3965 hydrochloride 相关产品

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生物活性

GW3965 hydrochloride is a potent and selective liver X receptor (LXR) agonist with EC₅₀s of 190 nM and 30 nM for hLXRα and hLXRβ, respectively^[1]^[2]^[3].

IC₅₀ & Target

EC50: 190 nM (hLXRα), 30 nM (hLXRβ)^[4]

体外研究
(In Vitro)

GW3965 hydrochloride promotes GBM cell death in vitro with enhanced efficacy in EGFRvIII-expressing tumor cells. GW3965 hydrochloride up-regulates expression of the cholesterol transporter gene ABCA1 and the E3 ubiquitin ligase IDOL and reduces LDLR levels^[2]. LXR ligands inhibits platelet aggregation and calcium mobilization stimulated by collagen or CRP. GW3965 hydrochloride (1 or 5 μM) displays a minor inhibitory effect on fibrinogen binding and P-selectin exposure, when platelets are stimulated with 1 μg/mL CRP. But using higher concentrations of GW3965 hydrochloride (10 μM) or T0901317 (40 μM), the levels of fibrinogen and P-selectin on the platelet surface are reduced^[3].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

GW3965 hydrochloride induces an increase of neuroactive steroids in the spinal cord, the cerebellum and the cerebral cortex of STZ-rats, but not in the CNS of non-pathological animals. GW3965 hydrochloride treatment induces an increase of dihydroprogesterone in the spinal cord of diabetic animals in association with an increase of myelin basic protein expression^[1]. GW3965 hydrochloride (40 mg/kg, p.o.) strongly induces ABCA1 expression and reduces LDLR expression, and this is accompanied by 59% inhibition of tumor growth, and a 25-fold increase in GBM cell apoptosis in vivo^[2]. GW3965 hydrochloride (2 mg/kg, i.v.) increases bleeding time and modulated platelet thrombus formation in vivo^[3].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

618.51

Formula

C₃₃H₃₂Cl₂F₃NO₃

CAS 号

405911-17-3

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据

In Vitro:

DMSO : 100 mg/mL (161.68 mM; Need ultrasonic)

H₂O : < 0.1 mg/mL (ultrasonic;warming;heat to 60°C) (insoluble)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.6168 mL	8.0839 mL	16.1679 mL
5 mM	0.3234 mL	1.6168 mL	3.2336 mL
10 mM	0.1617 mL	0.8084 mL	1.6168 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

1.

请依序添加每种溶剂： corn oil

Solubility: 10 mg/mL (16.17 mM); Suspended solution; Need ultrasonic
2.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline

Solubility: ≥ 2.5 mg/mL (4.04 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (4.04 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
3.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)

Solubility: 2.5 mg/mL (4.04 mM); Suspended solution; Need ultrasonic

此方案可获得 2.5 mg/mL (4.04 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。

以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
4.

请依序添加每种溶剂： 10% DMSO 90% corn oil

Solubility: ≥ 2.5 mg/mL (4.04 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (4.04 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在上海金畔生物科技有限公司网站选购。

参考文献

[1]. Mitro, Nico., et al. LXR and TSPO as new therapeutic targets to increase the levels of neuroactive steroids in the central nervous system of diabetic animals. Neurochemistry International (2012), 60(6), 616-621.

[2]. Guo, Deliang., et al. An LXR Agonist Promotes Glioblastoma Cell Death through Inhibition of an EGFR/AKT/SREBP-1/LDLR-Dependent Pathway. Cancer Discovery (2011), 1(5), 442-456.

[3]. Spyridon, Michael., et al. LXR as a novel antithrombotic target. Blood (2011), 117(21), 5751-5761.

[4]. Collins JL, et al. Identification of a nonsteroidal liver X receptor agonist through parallel array synthesis of tertiary amines. J Med Chem. 2002 May 9;45(10):1963-6.

Cell Assay ^[2]	Cells are seeded in 96 wells and are treated after 24 hours with different drugs indicated in each experiment in medium containing 1% FBS or lipoprotein deficient serum. Relative proliferation is determined using Cell Proliferation Assay Kit. Cells are incubated 1.5 hrs after adding tetrazolium salt WST-1 [2-(4-iodophenyl)-3- (4-nitrophenyl)-5-(2, 4-disulfo-phenyl)-2H-tetrazolium, monosodium salt] at 5% CO₂, 37ºC and the absorbance of the treated and untreated cells are measured using a microplate reader at 420 to 480 nm. Cells seeded in 12 well plates are counted using a hemocytometer, and dead cells are assessed using trypan blue exclusion assays. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[1]	Diabetes is induced in two-month-old male rats by a single i.p. injection of freshly prepared STZ (65 mg/kg) in 0.09 M citrate buffer, pH 4.8. Control animals are injected with 0.09 mol/L citrate buffer at pH 4.8. Hyperglycemia is confirmed 48 h after streptozotocin injection by measuring tail vein blood glucose levels using a glucometer OneTouch Ultra2. Only animals with mean plasma glucose levels over 300 mg/mL are classified as diabetic. Glycemia is also assessed before treatment with Ro5-4864 or GW3965 hydrochloride and before death. Two months after STZ injection, diabetic animals are treated once a week with Ro5-4864 (3 mg/kg) or GW3965 hydrochloride (50 mg/kg). Thus, they receive four subcutaneous injections in a month. Control diabetic rats receive 200 μL of vehicle (sesame oil). Four-month-old non-diabetic male rats are injected, following the same experimental schedule, with Ro5-4864, GW3965 hydrochloride or vehicle. Rats are killed 24 h after the last treatment. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献	[1]. Mitro, Nico., et al. LXR and TSPO as new therapeutic targets to increase the levels of neuroactive steroids in the central nervous system of diabetic animals. Neurochemistry International (2012), 60(6), 616-621. [2]. Guo, Deliang., et al. An LXR Agonist Promotes Glioblastoma Cell Death through Inhibition of an EGFR/AKT/SREBP-1/LDLR-Dependent Pathway. Cancer Discovery (2011), 1(5), 442-456. [3]. Spyridon, Michael., et al. LXR as a novel antithrombotic target. Blood (2011), 117(21), 5751-5761. [4]. Collins JL, et al. Identification of a nonsteroidal liver X receptor agonist through parallel array synthesis of tertiary amines. J Med Chem. 2002 May 9;45(10):1963-6.

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GW 501516(Synonyms: GW 1516; GSK-516)

发表于2024年9月30日由上海金畔生物科技有限公司

GW 501516 (Synonyms: GW 1516; GSK-516) 纯度: 99.15%

GW 501516 (GW 1516) 是 PPARδ 的激动剂，EC₅₀ 值为 1.1 nM。

GW 501516 Chemical Structure

CAS No. : 317318-70-0

规格	价格	是否有货
Free Sample (0.1-0.5 mg)		Apply now
10 mM * 1 mL in DMSO	￥495	In-stock
5 mg	￥450	In-stock
10 mg	￥730	In-stock
50 mg	￥1750	In-stock
100 mg	￥2400	In-stock
200 mg		询价
500 mg		询价

* Please select Quantity before adding items.

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Targeted Diversity Library

生物活性

GW 501516 (GW 1516) is a PPARδ agonist with an EC₅₀ of 1.1 nM^[1].

IC₅₀ & Target^[1]

PPARδ

1.1 nM (EC₅₀)

体外研究
(In Vitro)

GW 501516 is shown to be the most potent and selective PPARδ agonists known with an EC₅₀ of 1.1 nM against PPARδ and 1000-fold selectivity over the other human subtypes, PPARα and-γ^[1]. GW 501516 exerts anti-inflammatory effects in mouse cultured proximal tubular (mProx) cells. GW 501516 inhibits palmitate- and TNFα-induced increases in MCP-1 mRNA expression in a dose-dependent manner^[3].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

GW 501516 causes impaired bone formation, leading to decreased BMD and deterioration of bone properties in OVX rats^[2]. GW 501516 attenuates interstitial inflammation and proximal tubular cell damage in a protein-overload mouse nephropathy model^[3]. GW 501516 treatment enhances running endurance and the proportion of succinate dehydrogenase (SDH)-positive muscle fibres in both trained and untrained mice^[4].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

分子量

453.50

Formula

C₂₁H₁₈F₃NO₃S₂

CAS 号

317318-70-0

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

In Vitro:

DMSO : ≥ 100 mg/mL (220.51 mM)

* “≥” means soluble, but saturation unknown.

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.2051 mL	11.0254 mL	22.0507 mL
5 mM	0.4410 mL	2.2051 mL	4.4101 mL
10 mM	0.2205 mL	1.1025 mL	2.2051 mL

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline

Solubility: ≥ 2.5 mg/mL (5.51 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (5.51 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)

Solubility: 2.5 mg/mL (5.51 mM); Suspended solution; Need ultrasonic

此方案可获得 2.5 mg/mL (5.51 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。

以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil

Solubility: ≥ 2.5 mg/mL (5.51 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (5.51 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在上海金畔生物科技有限公司网站选购。

参考文献

[1]. Wei ZL, et al. A short and efficient synthesis of the pharmacological research tool GW501516 for the peroxisome proliferator-activated receptor delta. J Org Chem. 2003 Nov 14;68(23):9116-8.

[2]. Mosti MP, et al. Effects of the peroxisome proliferator-activated receptor (PPAR)-δ agonist GW 501516 on bone and muscle in ovariectomized rats. Endocrinology. 2014 Jun;155(6):2178-89.

[3]. Yang X, et al. GW 501516, a PPARδ agonist, ameliorates tubulointerstitial inflammation in proteinuric kidney disease via inhibition of TAK1-NFκB pathway in mice. PLoS One. 2011;6(9):e25271.

[4]. Chen W, et al. A metabolomic study of the PPARδ agonist GW 501516 for enhancing running endurance in Kunming mice. Sci Rep. 2015 May 6;5:9884.

[5]. Ji Y, et al. PPARβ/δ Agonist GW501516 Inhibits Tumorigenicity of Undifferentiated Nasopharyngeal Carcinoma in C666-1 Cells by Promoting Apoptosis. Front Pharmacol. 2018 Jun 28;9:648.

Cell Assay ^[3]	GW 501516 is dissolved in DMSO. Cells are starved by incubation in 0.2% FCS DMEM for 9 h, then pre-incubated with GW 501516, at a final concentration of 2.5 and 5 µM, or 0.05% DMSO as control for 3 hours, followed by stimulation with 150 µM palmitate bound to 8.0% BSA for 12 h^[3]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[2]^[3]	Rats: Female Sprague Dawley rats, 12 weeks of age, are allocated to a sham-operated group and 3 OVX groups; high-dose GW 501516 (OVX-GW5), low-dose GW 501516 (OVX-GW1), and a control group (OVX-CTR), respectively. Animals receive GW 501516 or vehicle (methylcellulose) daily for 4 months by gavage. Bone mineral density (BMD) is assessed by dual x-ray absorptiometry at the femur, spine, and whole body^[2]. Mice: Mice are randomly allocated to different groups and receive therapeutic diet and treatment. The GW 501516-containing rodent diet is made by evenly adding GW 501516 to the control diet to a final concentration of 0.04% w/w. In the control diet, 10% of the total calories are from fat (5.5% from soybean oil and 4.5% from lard)^[3]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献	[1]. Wei ZL, et al. A short and efficient synthesis of the pharmacological research tool GW501516 for the peroxisome proliferator-activated receptor delta. J Org Chem. 2003 Nov 14;68(23):9116-8. [2]. Mosti MP, et al. Effects of the peroxisome proliferator-activated receptor (PPAR)-δ agonist GW 501516 on bone and muscle in ovariectomized rats. Endocrinology. 2014 Jun;155(6):2178-89. [3]. Yang X, et al. GW 501516, a PPARδ agonist, ameliorates tubulointerstitial inflammation in proteinuric kidney disease via inhibition of TAK1-NFκB pathway in mice. PLoS One. 2011;6(9):e25271. [4]. Chen W, et al. A metabolomic study of the PPARδ agonist GW 501516 for enhancing running endurance in Kunming mice. Sci Rep. 2015 May 6;5:9884. [5]. Ji Y, et al. PPARβ/δ Agonist GW501516 Inhibits Tumorigenicity of Undifferentiated Nasopharyngeal Carcinoma in C666-1 Cells by Promoting Apoptosis. Front Pharmacol. 2018 Jun 28;9:648.

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GW2580

发表于2024年7月25日由上海金畔生物科技有限公司

GW2580 纯度: 99.83%

GW2580 是口服有效的，选择性的 c-Fms 激酶抑制剂，体外实验中在 0.06 μM 时可完全抑制人 cFMS 激酶。GW2580 是 ATP 与 cFMS 激酶结合的竞争性抑制剂，并且可以抑制集落刺激因子 1 信号传导。

GW2580 Chemical Structure

CAS No. : 870483-87-7

规格	价格	是否有货
Free Sample (0.1-0.5 mg)		Apply now
10 mM * 1 mL in DMSO	￥825	In-stock
10 mg	￥750	In-stock
50 mg	￥2200	In-stock
100 mg	￥3500	In-stock
200 mg	￥5500	In-stock
500 mg	￥11000	In-stock
1 g	￥16000	In-stock
5 g		询价
10 g		询价

* Please select Quantity before adding items.

GW2580 相关产品

•相关化合物库:

Bioactive Compound Library Plus
Immunology/Inflammation Compound Library
Kinase Inhibitor Library
Protein Tyrosine Kinase Compound Library
Anti-Cancer Compound Library
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生物活性

GW2580 is an orally bioavailable and selective inhibitor of c-Fms kinase which completely inhibits human cFMS kinase in vitro at 0.06 μM. GW2580 acts as a competitive inhibitor of ATP binding to the cFMS kinase and inhibits colony-stimulating-factor-1 signaling^[1].

IC₅₀ & Target

IC50: 60 nM (c-FMS)

体外研究
(In Vitro)

GW2580 completely inhibits the growth of CSF-1-dependent mouse myeloid M-NFS-60 cells at 0.7 μM. GW2580 at 0.8-1 μM completely blocks the ability of CSF-1 to induce the growth of mouse M-NFS60 myeloid cells and human monocytes^[1].
GW2580 causes a 30-40% inhibition of PTH-induced calcium release at 0.1-0.3 μM, with higher concentrations of 1, 3, and 10 μM completely inhibiting the PTH response^[1].
GW2580 inhibits CSF1R phosphorylation in RAW264.7 murine macrophages stimulated with 10 ng/mL with IC₅₀ of approximately 10 nM^[2].
GW2580 also inhibits TRKA activity with IC₅₀ of 0.88 μM^[3].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

GW2580 (Oral administration; 20 and 80 mg/kg) produces a dose-related decrease in the number of tumor cells, with the 80 mg/kg dose completely blocking tumor growth^[1].
GW2580 (Oral administration; 20 and 80 mg/kg) has gave maximal plasma concentrations of 1.4 and 5.6 μM, respectively^[1].
GW2580 (50 mg/kg; twice a day from days 0 to 21, 7 to 21, or 14 to 21) inhibits joint connective tissue and bone destruction in a 21-day adjuvant arthritis model^[3].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Female C3H/HEN mice or female CD-1 nude mice weighing 22-26 g^[1]
Dosage:	20 and 80 mg/kg
Administration:	Oral administration
Result:	Produced a dose-related decrease in the number of tumor cells, with the 80 mg/kg dose completely blocking tumor growth.

Animal Model:	Female C3H/HEN mice or female CD-1 nude mice weighing 22-26 g^[1]
Dosage:	20 and 80 mg/kg (Pharmacokinetic Study)
Administration:	Oral administration
Result:	Had gave maximal plasma concentrations of 1.4 and 5.6 μM, respectively.

分子量

366.41

Formula

C₂₀H₂₂N₄O₃

CAS 号

870483-87-7

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

In Vitro:

DMSO : 17.5 mg/mL (47.76 mM; Need ultrasonic and warming)

Ethanol : < 1 mg/mL (insoluble)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.7292 mL	13.6459 mL	27.2918 mL
5 mM	0.5458 mL	2.7292 mL	5.4584 mL
10 mM	0.2729 mL	1.3646 mL	2.7292 mL

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline

Solubility: ≥ 2.08 mg/mL (5.68 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (5.68 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)

Solubility: ≥ 2.08 mg/mL (5.68 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (5.68 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil

Solubility: ≥ 2.08 mg/mL (5.68 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (5.68 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在上海金畔生物科技有限公司网站选购。

参考文献

[1]. Conway JG, et al. Inhibition of colony-stimulating-factor-1 signaling in vivo with the orally bioavailable cFMS kinase inhibitor GW2580. Proc Natl Acad Sci U S A. 2005 Nov 1;102(44):16078-83.

[2]. Priceman SJ, et al. Targeting distinct tumor-infiltrating myeloid cells by inhibiting CSF-1 receptor: combating tumor evasion of antiangiogenic therapy. Blood. 2010 Feb 18;115(7):1461-71

[3]. Conway JG, et al. Effects of the cFMS kinase inhibitor 5-(3-methoxy-4-((4-methoxybenzyl)oxy)benzyl)pyrimidine-2,4-diamine (GW2580) in normal and arthritic rats. J Pharmacol Exp Ther. 2008 Jul;326(1):41-50.

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GW0742(Synonyms: GW610742)

发表于2024年7月23日由上海金畔生物科技有限公司

GW0742 (Synonyms: GW610742) 纯度: 99.47%

GW0742 是一种有效的 PPARβ 和 PPARδ 激动剂，在蛋白质结合实验中，对人 PPARδ 的 IC₅₀ 值为 1 nM；同时对人 PPARδ，PPARα 和 PPARγ 的 EC₅₀ 值分别为 1 nM，1.1 μM 和 2 μM。

GW0742 Chemical Structure

CAS No. : 317318-84-6

规格	价格	是否有货
Free Sample (0.1-0.5 mg)		Apply now
10 mM * 1 mL in DMSO	￥660	In-stock
5 mg	￥600	In-stock
10 mg	￥950	In-stock
50 mg	￥2950	In-stock
100 mg	￥5200	In-stock
200 mg		询价
500 mg		询价

* Please select Quantity before adding items.

GW0742 相关产品

•相关化合物库:

Bioactive Compound Library Plus
Cell Cycle/DNA Damage Compound Library
Immunology/Inflammation Compound Library
Anti-Cancer Compound Library
Anti-Aging Compound Library
Diabetes Related Compound Library
Anti-Cardiovascular Disease Compound Library
Pyroptosis Compound Library
Anti-Obesity Compound Library
Transcription Factor Targeted Library
Lipid Metabolism Compound Library

生物活性

GW0742 is a potent PPARβ and PPARδ agonist, with an IC₅₀ of 1 nM for human PPARδ in binding assay, and EC₅₀s of 1 nM, 1.1 μM and 2 μM for human PPARδ, PPARα, and PPARγ, respectively.

IC₅₀ & Target^[1]

PPARδ

1 nM (EC₅₀)

PPARα

1.1 μM (EC₅₀)

PPARγ

2 μM (EC₅₀)

体外研究
(In Vitro)

GW0742 is a potent PPARβ and PPARδ agonist, with an IC₅₀ of 1 nM for human PPARδ, and EC₅₀s of 1 nM, 1.1 μM and 2 μM for human PPARδ, PPARα, and PPARγ respectively^[1]. GW0742 (100 μM) activates human PPARα and mouse PPARβ in MCF-7 cells. GW0742 (100 μM) significantly reduces low-KCl-induced apoptosis of cerebellar granule neurons. GW0742 shows no obvious inherent toxicity on cerebellar granule neuronal cells after treatment of 3-100 μM for 24 h, but induces increased cell death at 100 μM after 48 hr of treatment. Moreover, GW0742 (100 μM) increases c-Jun expression in cerebellar granule neuron cultures observed at 6 hr^[2]. GW0742 (1 μM) induces PPARδ protein in neonatal rat cardiomyocytes. GW0742 also raises mRNA levels of long-chain acyl-CoA dehydrogenase (LCAD), very long-chain acyl-CoA dehydrogenase (VLCAD), acyl-CoA oxidase 1 (ACOX1), uncoupling protein 3 (UCP3), malonyl-CoA decarboxylase (MCD), and pyruvate dehydrogenase kinase 4 (PDK4) in neonatal rat cardiomyocytes^[4].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

GW0742 (0.3 mg/kg, i.p.) reduces intensity masson-trichrome staining, and attenuates the histological signs in bleomycin instillatio (BLEO)-induced lung injury of mice. GW0742 (0.3 mg/kg, i.p.) also causes a reduction of the BLEO-induced loss body weight, and a decrease of myeloperoxidase (MPO) activity. GW0742 shows significant inhibition of TNF-a and IL-1β in instilled-mice. GW0742 prevents bleomycin-induced IkB-a degradation, reduces the levels of NF-kB p65 in the lung, and decreases iNOS and p-ERK expression in BLEO-induced mice^[3]. GW0742 (5 mg/kg/day, i.v.) increases PPARδ protein level in the heart of rats. GW0742 also induces the increase in LCAD, VLCAD, and ACOX1 in the heart of rats^[4].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

471.49

Formula

C₂₁H₁₇F₄NO₃S₂

CAS 号

317318-84-6

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

In Vitro:

DMSO : ≥ 34 mg/mL (72.11 mM)

* “≥” means soluble, but saturation unknown.

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.1209 mL	10.6047 mL	21.2094 mL
5 mM	0.4242 mL	2.1209 mL	4.2419 mL
10 mM	0.2121 mL	1.0605 mL	2.1209 mL

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline

Solubility: ≥ 2.5 mg/mL (5.30 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (5.30 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% corn oil

Solubility: ≥ 2.5 mg/mL (5.30 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (5.30 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在上海金畔生物科技有限公司网站选购。

参考文献

[1]. Sznaidman ML, et al. Novel selective small molecule agonists for peroxisome proliferator-activated receptor delta (PPARdelta)–synthesis and biological activity. Bioorg Med Chem Lett. 2003 May 5;13(9):1517-21.

[2]. Smith SA, et al. Effect of the peroxisome proliferator-activated receptor beta activator GW0742 in rat cultured cerebellar granule neurons. J Neurosci Res. 2004 Jul 15;77(2):240-9.

[3]. Galuppo M, et al. GW0742, a high affinity PPAR-β/δ agonist reduces lung inflammation induced by bleomycin instillation in mice. Int J Immunopathol Pharmacol. 2010 Oct-Dec;23(4):1033-46.

[4]. Kuo SC, et al. Activation of receptors δ (PPARδ) by agonist (GW0742) may enhance lipid metabolism in heart both in vivo and in vitro. Horm Metab Res. 2013 Nov;45(12):880-6.

Cell Assay ^[2]	The PPARβ activator GW0742 and the RXR activator 9-cis-retinoic acid are dissolved in DMSO. The final DMSO concentration des not exceed 0.5% v/v, and this concentration is used in control wells. For each culture plate, one row of wells is treated with 500 μM glutamate. These wells serve as a positive control and for normalisation of data. Cell death (toxicity) is assessed by using an assay designed to measure lactate dehydrogenase (LDH) release^[2]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[3]	Male CD mice (25-35 g) are housed in a controlled environment and provided with standard rodent chow and water. Mice are randomized into four experimental groups: bleomycin-treated group: mice are subjected to lung injury induced by intratracheal instillation of bleomycin and treated daily via intraperitoneal injection with vehicle of GW0742 (10% dimethylsulfoxide (OMSO, 1 mL/kg), 1 h after BLEO instillation (n = 15). GW0742 group: identical to bleomycin-treated group but mice are treated daily with GW0742 (0.3 mg/kg, 1h after BLEO instillation) via intraperitoneal injection (n = 15). Sham-operated mice + vehicle group: animals are subjected to the identical surgical procedure but receive intratracheal instillation of saline (0.9%) instead of BLEO and are treated daily with the vehicle of GW0742 (10% dimethylsulfoxide (DMSO), 1 mL/kg, i.p.), 1 h after saline instillation (n = 15). Sham-operated mice + GW0742 group: identical to sham + vehicle group but mice are treated daily with GW0742 (0.3 mg/kg, 1 h after saline instillation) via intraperitoneal injection (n = 15)^[3]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献	[1]. Sznaidman ML, et al. Novel selective small molecule agonists for peroxisome proliferator-activated receptor delta (PPARdelta)–synthesis and biological activity. Bioorg Med Chem Lett. 2003 May 5;13(9):1517-21. [2]. Smith SA, et al. Effect of the peroxisome proliferator-activated receptor beta activator GW0742 in rat cultured cerebellar granule neurons. J Neurosci Res. 2004 Jul 15;77(2):240-9. [3]. Galuppo M, et al. GW0742, a high affinity PPAR-β/δ agonist reduces lung inflammation induced by bleomycin instillation in mice. Int J Immunopathol Pharmacol. 2010 Oct-Dec;23(4):1033-46. [4]. Kuo SC, et al. Activation of receptors δ (PPARδ) by agonist (GW0742) may enhance lipid metabolism in heart both in vivo and in vitro. Horm Metab Res. 2013 Nov;45(12):880-6.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

GW 5074

发表于2024年7月4日由上海金畔生物科技有限公司

GW 5074 纯度: 99.49%

GW 5074 是一种有效的，选择性的 c-Raf 抑制剂，IC₅₀ 值为 9 nM；对 JNK1/2/3，MEK1，MKK6/7，CDK1/2，c-Src，p38 MAP，VEGFR2 或 c-Fms 等没有作用。

GW 5074 Chemical Structure

CAS No. : 220904-83-6

规格	价格	是否有货
Free Sample (0.1-0.5 mg)		Apply now
10 mM * 1 mL in DMSO	￥1241	In-stock
5 mg	￥1083	In-stock
10 mg	￥1650	In-stock
50 mg	￥4848	In-stock
100 mg	￥5708	In-stock
200 mg		询价
500 mg		询价

* Please select Quantity before adding items.

GW 5074 相关产品

•相关化合物库:

Bioactive Compound Library Plus
Apoptosis Compound Library
Immunology/Inflammation Compound Library
Kinase Inhibitor Library
MAPK Compound Library
Anti-Cancer Compound Library
Oxygen Sensing Compound Library
Ferroptosis Compound Library
Glutamine Metabolism Compound Library
Anti-Pancreatic Cancer Compound Library
Anti-Liver Cancer Compound Library
Anti-Colorectal Cancer Compound Library

生物活性

GW 5074 is a potent and selective c-Raf inhibitor with IC₅₀ of 9 nM, and has no effect on the activities of JNK1/2/3, MEK1, MKK6/7, CDK1/2, c-Src, p38 MAP, VEGFR2 or c-Fms^[1]^[2].

IC₅₀ & Target

c-Raf

9 nM (IC₅₀)

体外研究
(In Vitro)

GW5074 is a potent and specific inhibitor of c-Raf with IC₅₀ of 9 nM and has no effect of MKK6, MKK7, p38 MAP kinase and cdks in vitro. However, treatment of neuronal cultures with GW5074 permits accumulation of activating modifications on c-Raf and also B-Raf. The inhibition of LK-induced apoptosis by GW5074 in cerebellar granule neurons is not MEK-ERK-dependent. GW5074 delays down-regulation of Akt activity but inhibits apoptosis by an Akt-independent mechanism. GW5074 affects Ras, nuclear factor-kappa B and c-jun. GW5074 inhibits cell death caused by neurotoxins in granule cells and other neuronal types^[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

GW5074 (5 mg/Kg) completely prevents extensive bilateral striatal lesions induced by 3-NP in mice^[1]. GW5074 suppresses sidestream smoke-induced airway hyperresponsiveness in mice^[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

520.94

Formula

C₁₅H₈Br₂INO₂

CAS 号

220904-83-6

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

In Vitro:

DMSO : ≥ 100 mg/mL (191.96 mM)

* “≥” means soluble, but saturation unknown.

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.9196 mL	9.5980 mL	19.1961 mL
5 mM	0.3839 mL	1.9196 mL	3.8392 mL
10 mM	0.1920 mL	0.9598 mL	1.9196 mL

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline

Solubility: ≥ 2.5 mg/mL (4.80 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (4.80 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

*以上所有助溶剂都可在上海金畔生物科技有限公司网站选购。

参考文献

[1]. Chin PC, et al. The c-Raf inhibitor GW5074 provides neuroprotection in vitro and in an animal model of neurodegeneration through a MEK-ERK and Akt-independent mechanism. J Neurochem, 2004, 90(3), 595-608.

[2]. Lei Y, et al. The Raf-1 inhibitor GW5074 and NSC 34521 suppress sidestream smoke-induced airway hyperresponsiveness in mice. Respir Res, 2008, 9(1), 71.

Kinase Assay ^[1]	Briefly, for each assay 5-10 mU of purified kinase is used. For GSK3β, cdk1, cdk2, cdk3, cdk5, the kinase is incubated with 1 μM GW5074 in a buffer containing 8 mM MOPS, pH 7.2, 0.2 mM EDTA, 10 mM magnesium acetate and [c-³³P-ATP] for 40 min at room temperature. Kinase activity is quantified by measuring ³³P incorporation by spotting an aliquot on P30 filters, washing in 50 mM phosphoric acid and scintillation counting. The buffer composition for c-Raf, JNK1, JNK2, JNK3, MEK1, MKK6, MKK7 is 50 mM Tris pH 7.5, 0.1 mM EGTA, 10 mM magnesium acetate and [c-³³P-ATP]. The peptide substrates used are as follows: For c-Raf, 0.66 mg/mL MBP; for cdks, 0.1 mg/mL histone H1; for JNKs, 3 μM ATF2; for MEK1, 1 μM MAPK2; for MKK6, 1 μM of SAPK2a and for MKK7, 2 μM JNK1α. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Assay ^[1]	Befiy, the tetrazolium salt MTT is added to the cultures at a final concentration of 1 mg/mL, and incubation of the culture is continued in the CO₂ incubator for a Hirther 30 min at 37°C. The assay is stopped by adding lysis buffer [20% sodium dodecyi sulfate (SDS) in 50% N,N-dimethyl formamide, pH 4.7], The absorbance is measured spectrophotometrically at 570 nm after an ovemight incubation at room temperature. The absorbance of a well without cells is used as background and subtracted. Data are presented as mean±standard deviation. Statistical analysis is perfomied using ANOVA and Student-Neuman-Keuls’ test. Besides MTT assays, viability is also quantitied using the tluorescein-diacetate method and by DAPI staining (which reveals apoptotic nuclei as condensed or fragmented). The results using these assays are similar to those obtained with the MTT assay. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[1]	The Tru-Scan^® activity monitoring system is used to assess locomotor activity on mice on the day following the 5 days of injection with saline, 3-NP or a combination of 3-NP and GW5074 (7 animals in each group). The animal is placed in a Perspex arena (25.9×25.9 cm) witb infrared beams spaced at 0.6-inch intervals in the X-Y plane. The arena is also equipped with a second infrared beam system at the Z plane positioned 2.54 cm above the X-Y plane. In this system the movement of the animal is accurately assessed by interruptions in 17×17-grid system created by the infrared beams in both the X-Y and Z planes. The animal is allowed to remain in the arena for 15 min, with data collection performed during this period using the Tru Scan Line interface box and Tm Scan 99 software, operating through a Pentium PC. The following behavioral parameters are selected: (i) Total movements episodes: each movement in the flor plane is a series of coordinate changes with no rest for at least I sample interval; (ii) total movement distance: the sum of all vectored A-Y coordinate changes in the floor plane; (iii) mean velocity: the mean velocity of all X-Y coordinate change defined movements; and (iv) vertical plane entries: the total number of times any part of the animal entered the vertical plane (Z plane). 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献	[1]. Chin PC, et al. The c-Raf inhibitor GW5074 provides neuroprotection in vitro and in an animal model of neurodegeneration through a MEK-ERK and Akt-independent mechanism. J Neurochem, 2004, 90(3), 595-608. [2]. Lei Y, et al. The Raf-1 inhibitor GW5074 and NSC 34521 suppress sidestream smoke-induced airway hyperresponsiveness in mice. Respir Res, 2008, 9(1), 71.

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GW284543(Synonyms: UNC10225170)

发表于2024年5月22日由上海金畔生物科技有限公司

GW284543 (Synonyms: UNC10225170) 纯度: 99.99%

GW284543 (UNC10225170) 是一个选择性的 MEK5 抑制剂。GW284543 (UNC10225170) 降低 pERK5，并下调内源性MYC 蛋白。

GW284543 Chemical Structure

CAS No. : 790186-68-4

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Free Sample (0.1-0.5 mg)		Apply now
10 mM * 1 mL in DMSO	￥1210	In-stock
5 mg	￥1100	In-stock
10 mg	￥1990	In-stock
50 mg	￥6900	In-stock
100 mg	￥9900	In-stock
200 mg		询价
500 mg		询价

* Please select Quantity before adding items.

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生物活性

GW284543 (UNC10225170) is a selective MEK5 inhibitor. GW284543 (UNC10225170) reduces pERK5, and decreases endogenous MYC protein^[1].

IC₅₀ & Target^[1]

MEK5

分子量

372.42

Formula

C₂₃H₂₀N₂O₃

CAS 号

790186-68-4

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

In Vitro:

DMSO : 125 mg/mL (335.64 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.6851 mL	13.4257 mL	26.8514 mL
5 mM	0.5370 mL	2.6851 mL	5.3703 mL
10 mM	0.2685 mL	1.3426 mL	2.6851 mL

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline

Solubility: ≥ 2.08 mg/mL (5.59 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (5.59 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)

Solubility: ≥ 2.08 mg/mL (5.59 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (5.59 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil

Solubility: ≥ 2.08 mg/mL (5.59 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (5.59 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在上海金畔生物科技有限公司网站选购。

参考文献

[1]. Vaseva AV, et al. KRAS Suppression-Induced Degradation of MYC Is Antagonized by a MEK5-ERK5 Compensatory Mechanism. Cancer Cell. 2018 Nov 12;34(5):807-822.e7.

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GW788388

发表于2024年5月2日由上海金畔生物科技有限公司

GW788388 纯度: 99.91%

GW788388 是一种有效的 ALK5 抑制剂，IC₅₀ 值 18 nM；同时抑制 TGF-β II 型受体和激活素 II 型受体的活性，但对 BMP II 型受体无作用。

GW788388 Chemical Structure

CAS No. : 452342-67-5

规格	价格	是否有货
10 mM * 1 mL in DMSO	￥671	In-stock
5 mg	￥610	In-stock
10 mg	￥990	In-stock
50 mg	￥3100	In-stock
100 mg	￥5200	In-stock
200 mg		询价
500 mg		询价

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生物活性

GW788388 is a potent and selective inhibitor of ALK5 with IC₅₀ of 18 nM, and also inhibits TGF-β type II receptor and activin type II receptor activities, without inhibiting BMP type II receptor.

IC₅₀ & Target

IC50: 18 nM (ALK5)

体内研究
(In Vivo)

GW788388 given orally for 5 weeks significantly reduces renal fibrosis and decreased the mRNA levels of key mediators of extracellular matrix deposition in kidneys in db/db mice^[1]. GW788388 (50 mg/kg/day, p.o.) significantly attenuates systolic dysfunction in the MI animals, together with the attenuation of the activated (phosphorylated) Smad2 (P < 0.01), α-smooth muscle actin (P < 0.001), and collagen I (P < 0.05) in the noninfarct zone of MI rats^[2]. GW788388 reduces the expression of collagen IA1 by 80% at a dose of 1 mg/kg twice a day (b.i.d.). GW788388 significantly reduces the expression of collagen IA1 mRNA when administered orally at 10 mg/kg once a day (u.i.d.) in a model of puromycin aminonucleoside-induced renal fibrosis^[3].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

425.48

Formula

C₂₅H₂₃N₅O₂

CAS 号

452342-67-5

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

In Vitro:

DMSO : ≥ 48 mg/mL (112.81 mM)

* “≥” means soluble, but saturation unknown.

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.3503 mL	11.7514 mL	23.5029 mL
5 mM	0.4701 mL	2.3503 mL	4.7006 mL
10 mM	0.2350 mL	1.1751 mL	2.3503 mL

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline

Solubility: ≥ 2.5 mg/mL (5.88 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (5.88 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)

Solubility: ≥ 2.5 mg/mL (5.88 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (5.88 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil

Solubility: ≥ 2.5 mg/mL (5.88 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (5.88 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在上海金畔生物科技有限公司网站选购。

参考文献

[1]. Petersen M, et al. Oral administration of GW788388, an inhibitor of TGF-beta type I and II receptor kinases, decreases renal fibrosis. Kidney Int, 2008, 73(6), 705-715.

[2]. Tan SM, et al. Targeted inhibition of activin receptor-like kinase 5 signaling attenuates cardiac dysfunction following myocardial infarction. Am J Physiol Heart Circ Physiol, 2010, 298(5), H1415-1425.

[3]. Gellibert F, et al. Discovery of 4-{4-[3-(pyridin-2-yl)-1H-pyrazol-4-yl]pyridin-2-yl}-N-(tetrahydro-2H- pyran-4-yl)benzamide (GW788388): a potent, selective, and orally active transforming growth factor-beta type I receptor inhibitor. J Med Chem. 2006, 49

Animal Administration
^[2]

One week postsurgery, sham-operated (N=6) and infarcted animals (N=10) are randomized to treatment with the ALK5 inhibitor GW788388 (GSK) at a dosage of 50 mg/kg/day by gavage, which has been shown to significantly attenuate collagen overexpression in a rodent model of dimethylnitrosamine-induced liver disease. Untreated rats, that is, sham-operated (N=9) and MI animals (N=15), are gavaged with vehicle (1% carboxymethyl cellulose solution). Four animals with < 25% infarct size as determined postmortem by histology are excluded from further analyses.

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

参考文献

[1]. Petersen M, et al. Oral administration of GW788388, an inhibitor of TGF-beta type I and II receptor kinases, decreases renal fibrosis. Kidney Int, 2008, 73(6), 705-715.

[2]. Tan SM, et al. Targeted inhibition of activin receptor-like kinase 5 signaling attenuates cardiac dysfunction following myocardial infarction. Am J Physiol Heart Circ Physiol, 2010, 298(5), H1415-1425.

[3]. Gellibert F, et al. Discovery of 4-{4-[3-(pyridin-2-yl)-1H-pyrazol-4-yl]pyridin-2-yl}-N-(tetrahydro-2H- pyran-4-yl)benzamide (GW788388): a potent, selective, and orally active transforming growth factor-beta type I receptor inhibitor. J Med Chem. 2006, 49

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Pazopanib Hydrochloride(Synonyms: 盐酸帕唑帕尼; GW786034 (Hydrochloride))

发表于2024年4月14日由上海金畔生物科技有限公司

Pazopanib Hydrochloride (Synonyms: 盐酸帕唑帕尼; GW786034 (Hydrochloride)) 纯度: 99.84%

Pazopanib Hydrochloride (GW786034 Hydrochloride) 是多靶点抑制剂，抑制 VEGFR1，VEGFR2，VEGFR3，PDGFRβ，c-Kit，FGFR1，c-Fms的IC₅₀分别为10，30，47，84，74，140，146 nM。

Pazopanib Hydrochloride Chemical Structure

CAS No. : 635702-64-6

规格	价格	是否有货
Free Sample (0.1-0.5 mg)		Apply now
10 mM * 1 mL in DMSO	￥572	In-stock
10 mg	￥520	In-stock
50 mg	￥1100	In-stock
100 mg	￥1600	In-stock
200 mg	￥2700	In-stock
500 mg	￥4500	In-stock
1 g		询价
5 g		询价

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生物活性

Pazopanib Hydrochloride (GW786034 Hydrochloride) is a novel multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFRβ, c-Kit, FGFR1, and c-Fms with an IC₅₀ of 10, 30, 47, 84, 74, 140 and 146 nM, respectively.

IC₅₀ & Target^[1]

VEGFR1

10 nM (IC₅₀)

VEGFR2

30 nM (IC₅₀)

VEGFR3

47 nM (IC₅₀)

PDGFRβ

84 nM (IC₅₀)

FGFR1

140 nM (IC₅₀)

c-Kit

74 nM (IC₅₀)

c-Fms

146 nM (IC₅₀)

体外研究
(In Vitro)

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

分子量

473.98

Formula

C₂₁H₂₄ClN₇O₂S

CAS 号

635702-64-6

中文名称

盐酸帕唑帕尼；帕唑帕尼盐酸盐

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据

In Vitro:

DMSO : 10 mg/mL (21.10 mM; Need ultrasonic)

H₂O : < 0.1 mg/mL (ultrasonic;warming;heat to 60°C) (insoluble)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.1098 mL	10.5490 mL	21.0979 mL
5 mM	0.4220 mL	2.1098 mL	4.2196 mL
10 mM	0.2110 mL	1.0549 mL	2.1098 mL

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline

Solubility: ≥ 1 mg/mL (2.11 mM); Clear solution

此方案可获得 ≥ 1 mg/mL (2.11 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 10.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)

Solubility: ≥ 1 mg/mL (2.11 mM); Clear solution

此方案可获得 ≥ 1 mg/mL (2.11 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 10.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil

Solubility: ≥ 1 mg/mL (2.11 mM); Clear solution

此方案可获得 ≥ 1 mg/mL (2.11 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

以 1 mL 工作液为例，取 100 μL 10.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在上海金畔生物科技有限公司网站选购。

参考文献

[1]. Harris PA, et al. Discovery of 5-[[4-[(2,3-dimethyl-2H-indazol-6-yl)methylamino]-2-pyrimidinyl]amino]-2-methyl-benzenesulfonamide (Pazopanib), a novel and potent vascular endothelial growth factor receptor inhibitor. J Med Chem. 2008, 51(15), 4632-4640.

[2]. Thakur A, et al. Pazopanib, a multitargeted tyrosine kinase inhibitor, reduces diabetic retinal vascular leukostasis and leakage. Microvasc Res. 2011 Nov;82(3):346-50.

Kinase Assay ^[1]	VEGFR enzyme assays are initiated by the addition of 10 μL of activated VEGFR2 kinase solution [final concentration, 1 nM enzyme in 0.1 M 4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid (HEPES), pH 7.5, containing 0.1 mg/mL bovine serum albumin (BSA), 300 μM dithiothreitol (DTT)] to 10 μL substrate solution [final concentration, 360 nM peptide, (biotin-aminohexyl-EEEEYFELVAKKKK-NH2), 75 μM ATP, 10 μM MgCl₂], and 1 μL of titrated compound (Pazopanib) in DMSO. Plates are incubated at room temperature for 60 min, and then the reaction is quenched by the addition of 20 μL of 100 mM ethylene diamine tetraacetic acid (EDTA). After quenching, 20 μL HTRF reagents (final concentration, 15 nM Streptavidin-linked allophycocyanin, 1 nM Europium-labeled antiphosphotyrosine antibody diluted in 0.1 mg/mL BSA, 0.1 M HEPES, pH 7.5) is added and the plates incubated for a minimum of 10 min. The fluorescence at 665 nM is measured with a plate reader^[1]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Assay ^[1]	The effect of Pazopanib on cell proliferation is measured using 5-bromo-2-deoxyuridine (BrdU) incorporation method using commercially available kits. HUVEC is seeded in medium containing 5% fetal bovine serum (FBS) in type 1 collagen coated 96-well plates and incubated overnight at 37°C, 5% CO₂. The medium is aspirated from the cells, and various concentrations of Pazopanib in serum-free medium are added to each well. After 30 min, either VEGF (10 ng/mL) or bFGF (0.3 ng/mL) is added to the wells. Cells are incubated for an additional 72 h and BrdU (10 μM) is added during the last 18 to 24 h of incubation. At the end of incubation, BrdU incorporation in cells is measured by ELISA. Data are fitted with a curve described by the equation, y=V_max(1−(x/(K+x))), where K is equal to the IC₅₀^[1]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[1]^[2]	Mice^[1] Tumors are initiated by injection of tumor cell suspension in 8−12 week old nude mice. When tumors reach a volume of 100−200 mm³, mice are randomized and divided into groups of eight. Pazopanib is administered once or twice daily at 10, 30, or 100 mg/kg. Animals are euthanized by inhalation of CO₂ at the completion of the study. Tumor volume is measured twice weekly by calipers, using the equation: tumor volume (mm³)=(length×width²)/2. Results are routinely reported as % inhibition=1−(average growth of the drug treated population/average growth of vehicle treated control population). Rats^[2] Male Brown-Norway (BN; pigmented) rats weighing 200 to 250 g are acclimatized for at least two days prior to any experimental procedure. After overnight fasting for 12-16 h, an intraperitoneal injection of 30 mg/mL solution of Streptozotocin in 10 mM citrate buffer (pH 4.5) is administered (60 mg/kg body weight) to induce diabetes. After 3-4 h of Streptozotocin injection, animals are put on a regular diet and 24 h after Streptozotocin injection, blood sample (5-10 μL) is collected via tail vein. The blood glucose levels in the animals are determined with a glucose monitor. Animals with blood glucose levels greater than 250 mg/dL are considered diabetic. The animals are divided into three groups. Group 1: Healthy (n=12), Group 2: Diabetic (n=12) and Group 3: Diabetic+Treatment (n=12). Treatment is started immediately after diabetes induction. Both eyes are dosed twice daily for 30 days with 0.5 % w/v Pazopanib suspension (10 μL volume in each eye) and animals in all groups are sacrificed on day 31, 16-17 h after last dose on day 30. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献	[1]. Harris PA, et al. Discovery of 5-[[4-[(2,3-dimethyl-2H-indazol-6-yl)methylamino]-2-pyrimidinyl]amino]-2-methyl-benzenesulfonamide (Pazopanib), a novel and potent vascular endothelial growth factor receptor inhibitor. J Med Chem. 2008, 51(15), 4632-4640. [2]. Thakur A, et al. Pazopanib, a multitargeted tyrosine kinase inhibitor, reduces diabetic retinal vascular leukostasis and leakage. Microvasc Res. 2011 Nov;82(3):346-50.

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Lapatinib ditosylate(Synonyms: 二甲苯磺酸拉帕替尼; GW572016 ditosylate; GW2016 ditosylate)

发表于2024年4月13日由上海金畔生物科技有限公司

Lapatinib ditosylate (Synonyms: 二甲苯磺酸拉帕替尼; GW572016 ditosylate; GW2016 ditosylate) 纯度: 99.95%

Lapatinib ditosylate (GW572016 ditosylate) 是一种 ErbB-2 和 EGFR 酪氨酸激酶结构域的有效抑制剂，对纯化的 EGFR 和 ErbB-2 的 IC₅₀ 值分别为 10.2 和 9.8 nM。

Lapatinib ditosylate Chemical Structure

CAS No. : 388082-77-7

规格	价格	是否有货
Free Sample (0.1-0.5 mg)		Apply now
10 mM * 1 mL in DMSO	￥770	In-stock
50 mg	￥700	In-stock
100 mg	￥1200	In-stock
500 mg	￥3000	In-stock
1 g	￥4500	In-stock
5 g		询价
10 g		询价

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Anti-Colorectal Cancer Compound Library

生物活性

Lapatinib ditosylate (GW572016 ditosylate) is a potent inhibitor of the ErbB-2 and EGFR tyrosine kinase domains with IC₅₀ values against purified EGFR and ErbB-2 of 10.2 and 9.8 nM, respectively^[1].

IC₅₀ & Target

EGFR

10.8 nM (IC₅₀, Cell Free Assay)

ErbB2

9.2 nM (IC₅₀, Cell Free Assay)

体外研究
(In Vitro)

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis^[1]

Cell Line:	BT474 and HN5 cells
Concentration:	0.03 µM, 0.1 µM, 0.3 µM, 1 µM, 3 µM, or 10 µM
Incubation Time:	6 hours
Result:	Inhibited receptor autophosphorylation of EGFR and ErbB-2 in a dose-responsive manner. Phosphorylation of serine 473 of AKT was also inhibited in a dose-dependent manner.

Cell Proliferation Assay^[1]

Cell Line:	HN5, A-43, BT474, N87, and CaLu-3 cells
Concentration:
Incubation Time:	72 hours
Result:	Inhibited the growth of tumor cells overexpressing EGFR or ErbB-2.

Cell Cycle Analysis^[1]

Cell Line:	HN5 cells
Concentration:	1 µM, or 10 µM
Incubation Time:	72 hours
Result:	Resulted in induction of G1 arrest.

体内研究
(In Vivo)

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	CD-1 nude female mice (4-6 weeks old) with HN5 cells^[1]
Dosage:	30 mg/kg, 100 mg/kg
Administration:	Oral administration; twice daily; for 21 days
Result:	Inhibited tumor xenograft growth of the HN5 cells in a dose-responsive manner.

Clinical Trial

分子量

925.46

Formula

C₄₃H₄₂ClFN₄O₁₀S₃

CAS 号

388082-77-7

中文名称

二甲苯磺酸拉帕替尼；二对甲苯磺酸拉帕替尼；拉帕替尼泊

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

溶解性数据

In Vitro:

DMSO : 125 mg/mL (135.07 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.0805 mL	5.4027 mL	10.8054 mL
5 mM	0.2161 mL	1.0805 mL	2.1611 mL
10 mM	0.1081 mL	0.5403 mL	1.0805 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline

Solubility: ≥ 2.33 mg/mL (2.52 mM); Clear solution

此方案可获得 ≥ 2.33 mg/mL (2.52 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 23.3 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)

Solubility: ≥ 2.33 mg/mL (2.52 mM); Clear solution

此方案可获得 ≥ 2.33 mg/mL (2.52 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 23.3 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明

*以上所有助溶剂都可在上海金畔生物科技有限公司网站选购。

参考文献

[1]. Rusnak DW, et al. The effects of the novel, reversible epidermal growth factor receptor/ErbB-2 tyrosine kinase inhibitor, GW2016, on the growth of human normal and tumor-derived cell lines in vitro and in vivo. Mol Cancer Ther. 2001 Dec;1(2):85-94

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GW 441756

发表于2024年4月12日由上海金畔生物科技有限公司

GW 441756 纯度: 98.65%

GW 441756 是一种高效特异性神经生长因子 (NGF) 受体酪氨酸激酶 a (TrkA) 抑制剂 (IC₅₀=2 nM)，可消除 BmK NSPK-induced 神经突生长。

GW 441756 Chemical Structure

CAS No. : 504433-23-2

规格	价格	是否有货
10 mM * 1 mL in DMSO	￥921	In-stock
10 mg	￥837	In-stock
50 mg	￥3464	In-stock
100 mg		询价
200 mg		询价

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GW 441756 相关产品

•相关化合物库:

Bioactive Compound Library Plus
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生物活性

GW 441756 is a potent and specific nerve growth factor (NGF) receptor tyrosine kinases A (TrkA) inhibitor (IC₅₀=2 nM), which eliminates the BmK NSPK-induced neurite outgrowth^[1]^[2]^[3].

IC₅₀ & Target^[1]

TrkA

2 nM (IC₅₀)

体外研究
(In Vitro)

GW-441756 (1 µM; 48 hours; spinal cord neurons cells) abolishs BmK NSPK-induced neurite outgrowth^[1].
GW-441756 (1 µM; 4 hours; PC12 cells) inhibits nerve growth factor induced neurite outgrowth^[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Immunofluorescence^[1]

Cell Line:	Spinal cord neurons cells
Concentration:	1 µM
Incubation Time:	48 hours
Result:	Abolished BmK NSPK-induced neurite outgrowth.

分子量

275.30

Formula

C₁₇H₁₃N₃O

CAS 号

504433-23-2

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

In Vitro:

DMSO : 17.5 mg/mL (63.57 mM; Need ultrasonic and warming)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	3.6324 mL	18.1620 mL	36.3240 mL
5 mM	0.7265 mL	3.6324 mL	7.2648 mL
10 mM	0.3632 mL	1.8162 mL	3.6324 mL

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline

Solubility: ≥ 2.08 mg/mL (7.56 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (7.56 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

*以上所有助溶剂都可在上海金畔生物科技有限公司网站选购。

参考文献

[1]. Zhao F, et al. BmK NSPK, a Potent Potassium Channel Inhibitor from Scorpion Buthus martensii Karsch, Promotes Neurite Outgrowth via NGF/TrkA Signaling Pathway. Toxins (Basel). 2021;13(1):33. Published 2021 Jan 5.

[2]. Terada K, et al. Cholinesterase inhibitor rivastigmine enhances nerve growth factor-induced neurite outgrowth in PC12 cells via sigma-1 and sigma-2 receptors. PLoS One. 2018;13(12):e0209250. Published 2018 Dec 17.

[3]. Wood ER, et al. Discovery and in vitro evaluation of potent TrkA kinase inhibitors: oxindole and aza-oxindoles. Bioorg Med Chem Lett. 2004;14(4):953-957.

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Pazopanib-d6(Synonyms: GW786034-d6)

发表于2024年3月18日由上海金畔生物科技有限公司

Pazopanib-d6 (Synonyms: GW786034-d6)

Pazopanib-d6 (GW786034-d6) 是 Pazopanib 的氘代物。Pazopanib (GW786034) 是多靶点抑制剂，抑制 VEGFR1，VEGFR2，VEGFR3，PDGFRβ，c-Kit，FGFR1，c-Fms的IC₅₀分别为10，30，47，84，74，140，146 nM。

Pazopanib-d6 Chemical Structure

CAS No. : 1219592-01-4

规格		是否有货
100 mg		询价
250 mg		询价
500 mg		询价

* Please select Quantity before adding items.

生物活性	Pazopanib-d6 (GW786034-d6) is the deuterium labeled Pazopanib. Pazopanib (GW786034) is a novel multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFRβ, c-Kit, FGFR1, and c-Fms with IC₅₀s of 10, 30, 47, 84, 74, 140 and 146 nM, respectively.
体外研究 (In Vitro)	Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs^[1]. Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量	443.55
Formula	C₂₁H₁₇D₆N₇O₂S
CAS 号	1219592-01-4
中文名称	帕唑帕尼 d6
运输条件	Room temperature in continental US; may vary elsewhere.
储存方式	Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献	[1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216. [2]. Harris PA, et al. Discovery of 5-[[4-[(2,3-dimethyl-2H-indazol-6-yl)methylamino]-2-pyrimidinyl]amino]-2-methyl-benzenesulfonamide (Pazopanib), a novel and potent vascular endothelial growth factor receptor inhibitor. J Med Chem. 2008, 51(15), 4632-4640. [3]. Thakur A, et al. Pazopanib, a multitargeted tyrosine kinase inhibitor, reduces diabetic retinal vascular leukostasis and leakage. Microvasc Res. 2011 Nov;82(3):346-50.

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上海实验高温系列电热鼓风干燥箱GW-3型

发表于2024年3月1日由上海金畔生物科技有限公司

上海实验高温系列电热鼓风干燥箱GW-3型

品牌上海实验仪器厂|SL

型号 GW-3

商品详情

上海实验高温系列电热鼓风干燥箱GW-3型

产品说明

本系列产品具有较大的温度选择范围，可满足对物品进行500℃以下的特殊需要的高温老化，温度试验及烘焙、干燥、热处理等（但不适用于对易燃易爆易挥发物品的干燥，以免发生爆炸）。

产品特征

1、采用数显温度仪表对工作室温度进行连续P.I.D调节控温，操作简便、直观，控温精度高；

2、外壳选用优质薄钢板制作，表面喷漆

3、工作室内胆选用不锈钢制成，耐高温、抗氧化性能好；

4、加热器采用优质电加热专用合金丝制作

5、硅酸铝（矿碴棉）作绝热保温层材料，保温效果好；

6、优良的风道设计，及强制空气循环方式，以提高温度均匀性；

7、具有超温声、光报警功能；配有电动机热保护，设备过流（载）断路保护装置。

技术参数

项　目	单位	型号
项　目	单位	GW-3	8810A
电加热器功率	kW	12	16
电源电压	V	380/220
相数频率		三相四线3-phase 4-wire 50Hz
工作温度范围	℃	100～500	室温+10～500
温度波动度	℃	≤±1.5	≤±1
工作室尺寸(D×W×H)	mm	500×600×750	800×800×1000
外形尺寸(D×W×H)	mm	920×1220×1380	1230×1430×1680
毛重	kg	350	630