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CKI-7 free base

发表于由

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。

CKI-7 free base  纯度: 99.31%

CKI-7 free base 是一种有效且 ATP 竞争性的酪蛋白激酶 1 (CK1) 抑制剂，IC50 为 6 μM，Ki 为 8.5 μM。CKI-7 free base 选择性抑制 Cdc7 激酶，还抑制 SGK，S6K1 以及 MSK1。CKI-7 free base 对酪蛋白激酶 II 和其他蛋白激酶的作用弱得多。

CKI-7 free base

CKI-7 free base Chemical Structure

CAS No. : 120615-25-0

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥1572 In-stock
5 mg ￥850 In-stock
10 mg ￥1500 In-stock
25 mg ￥3750 In-stock
50 mg ￥6250 In-stock
100 mg ￥11200 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

CKI-7 free base 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus
  • Cell Cycle/DNA Damage Compound Library
  • Immunology/Inflammation Compound Library
  • Kinase Inhibitor Library
  • MAPK Compound Library
  • Metabolism/Protease Compound Library
  • Stem Cell Signaling Compound Library
  • Wnt/Hedgehog/Notch Compound Library
  • Anti-Cancer Compound Library
  • Anti-Aging Compound Library
  • Reprogramming Compound Library
  • Oxygen Sensing Compound Library
  • Glutamine Metabolism Compound Library
  • Anti-Breast Cancer Compound Library
  • Anti-Blood Cancer Compound Library
  • Anti-Cancer Metabolism Compound Library

生物活性

CKI-7 free base is a potent and ATP-competitive casein kinase 1 (CK1) inhibitor with an IC50 of 6 μM and a Ki of 8.5 μM. CKI-7 free base is a selective Cdc7 kinase inhibitor. CKI-7 free base also inhibits SGK, ribosomal S6 kinase-1 (S6K1) and mitogen- and stress-activated protein kinase-1 (MSK1). CKI-7 free base has a much weaker effect on casein kinase II and other protein kinases[1][2][3][4].

IC50 & Target[1][2][3]

CK1

6 μM (IC50)

CK1

8.5 μM (Ki)

Cdc7

 

SGK

 

S6K1

 

MSK1

 

体外研究
(In Vitro)

CKI-7 (0.1-10 μM; 5 days; ES cells) treatment significantly increases the expression of the early neuroectodermal marker Sox1 and the number of cells positive for the neural markers nestin and βIII-tubulin, in a concentration-dependent manner[1].
CKI-7 (5 μM; 5 days; ES cells) treatment suppresses SFEB-induced β-catenin stabilization on day 5, indicating that CKI-7 inhibits Wnt signaling[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.

RT-PCR[1]

Cell Line: Mouse ES cells
Concentration: 0.1-10 μM
Incubation Time: 5 days
Result: Significantly increased the expression of the early neuroectodermal marker Sox1 and the number of cells positive for the neural markers nestin and βIII-tubulin, in a concentration-dependent manner.

Western Blot Analysis[1]

Cell Line: Mouse ES cells
Concentration: 5 μM
Incubation Time: 5 days
Result: Suppressed SFEB-induced β-catenin stabilization on day 5.

体内研究
(In Vivo)

In vivo dose-dependent anti-tumor activity of CKI-7 is demonstrated in a SCID-Beige mouse systemic tumor model utilzing a recently isolated Philadelphia chromosome positive acute lymphoblastic leukemia cell line. Standard cell cycle synchronization studies established that exposure to CKI-7 results in cell cycle dependent caspase 3 activation and apoptotic cell death[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

285.75

Formula

C11H12ClN3O2S
CAS 号

120615-25-0
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 : 25 mg/mL (87.49 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.4996 mL 17.4978 mL 34.9956 mL
5 mM 0.6999 mL 3.4996 mL 6.9991 mL
10 mM 0.3500 mL 1.7498 mL 3.4996 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: ≥ 2.08 mg/mL (7.28 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (7.28 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 (7.28 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (7.28 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 (7.28 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (7.28 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]. Osakada F, et al. In vitro differentiation of retinal cells from human pluripotent stem cells by small-molecule induction. J Cell Sci. 2009 Sep 1;122(Pt 17):3169-79.

    [2]. Mark G. Frattini, et al. Small Molecule Inhibition of Cdc7, a Key Cell Cycle Regulator and Novel Therapeutic Target, Successfully Inhibits Leukemia Cell Growth in Vitro and in Vivo. Blood (2008) 112 (11): 2668.

    [3]. Chijiwa T, et al. A newly synthesized selective casein kinase I inhibitor, N-(2-aminoethyl)-5-chloroisoquinoline-8-sulfonamide, and affinity purification of casein kinase I from bovine testis. J Biol Chem. 1989 Mar 25;264(9):4924-7.

    [4]. Rena G, et al. D4476, a cell-permeant inhibitor of CK1, suppresses the site-specific phosphorylation and nuclear exclusion of FOXO1a. EMBO Rep. 2004 Jan;5(1):60-5.

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

LY-2584702 free base

发表于由

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。

LY-2584702 free base 

LY-2584702 free base 是一种 ATP 竞争性的选择性 p70S6K 抑制剂，IC50 为 4 nM。LY-2584702 抑制 S6K1 的 IC50 为 2 nM。

LY-2584702 free base

LY-2584702 free base Chemical Structure

CAS No. : 1082949-67-4

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

* Please select Quantity before adding items.

LY-2584702 free base 的其他形式现货产品:

LY-2584702 tosylate salt

生物活性

LY-2584702 free base is a selective ATP competitive inhibitor of p70S6K with an IC50 of 4 nM. In S6K1 enzyme assay, the IC50 of LY-2584702 is 2 nM.

IC50 & Target[1][2]

S6K1

2 nM (IC50)

p70S6K

4 nM (IC50)

体外研究
(In Vitro)

LY-2584702 (LY2584702) inhibits phosphorylation of the S6 ribosomal protein (pS6) in HCT116 colon cancer cells with an IC50 of 0.1-0.24 μM[1]. For pS6 inhibition in cells, the IC50=100 nM. LY-2584702 has some activity against the S6K-related kinases MSK2 and RSK at high concentrations (enzyme assay IC50=58-176 nM). LY-2584702 inhibits S6K activity in EOMA cells, as determined by the phosphorylation of its downstream effector S6, in a dose-dependent manner[2]. Proliferation of A549 is significantly inhibited by LY-2584702 (LY2584702) treating over 24 h at 0.1 μM (P<0.05); and the trend of decline is more conspicuous with longer treatment and/or with the increased drug concentration (all P<0.05). Similar results are also observed in SK-MES-1, although the obvious inhibition is led by LY-2584702 at 0.6 μM (P<0.05), much higher than that of A549[3].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究
(In Vivo)

LY-2584702 demonstrates significant single-agent efficacy in both U87MG glioblastoma and HCT116 colon carcinoma xenograft models at two dose levels of 2.5 mg/kg twice daily (BID) and 12.5 mg/kg BID. LY-2584702 demonstrates statistically significant tumour growth reduction at TMED50 (threshold minimum effective dose 50%) (2.3 mg/kg) and TMED90 (10 mg/kg) in the HCT116 colon carcinoma xenograft model[1]. To examine the role of S6K in vivo, EOMA cells expressing shAkt3 are implanted in nu/nu mice, then treated for 14 days with LY-2584702 or Rapamycin. Analysis of tumors removed after 14 days shows that LY-2584702 inhibits S6 phosphorylation almost as effectively as Rapamycin. Loss of Akt3 increases tumor growth as compared with pLKO. LY-2584702 treatment alone does not significantly affect the growth of pLKO tumors. However, LY-2584702 significantly reduces the growth of tumors with shAkt3[2].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial

分子量

445.42

Formula

C21H19F4N7
CAS 号

1082949-67-4
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 : ≥ 4.5 mg/mL (10.10 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 2.2451 mL 11.2254 mL 22.4507 mL
5 mM 0.4490 mL 2.2451 mL 4.4901 mL
10 mM 0.2245 mL 1.1225 mL 2.2451 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。
参考文献

  • [1]. Tolcher A, et al. A phase I trial of LY2584702 tosylate, a p70 S6 kinase inhibitor, in patients with advanced solid tumors. Eur J Cancer. 2014 Mar;50(5):867-75.

    [2]. Phung TL, et al. Akt1 and akt3 exert opposing roles in the regulation of vascular tumor growth. Cancer Res. 2015 Jan 1;75(1):40-50.

    [3]. Chen B, et al. Hyperphosphorylation of RPS6KB1, rather than overexpression, predicts worse prognosis in non-small cell lung cancer patients. PLoS One. 2017 Aug 9;12(8):e0182891.
Cell Assay
[3]

LY-2584702 is fully dissolved in 20 mL 10% DMSO and reserved at -80°C. When conducted the experiments in vitro, LY-2584702 is further diluted in 0.5% Tween 80, 5% propylene glycol and 30% PEG400 to reach different DMSO concentrations of 0.1 μM, 0.2 μM, 0.6 μM, and 1.0 μM. Cell Counting Kit-8 (CCK-8) is used to measure the cells proliferation in vitro. Cell lines A549 and SK-MES-1 treated by LY-2584702 for 24 h with different concentrations are seeded in 96-well plates at a density of 5×103 per well, with six repeats. DMSO treated, or in other words, the concentration of LY-2584702 of 0 is used as negative control. Cells absorbance at 450 nm is detected every 24 h after seeding to measure the proliferative activities[3].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[2]

Mice[2]
LY-2584702 is prepared in 0.25% Tween-80 and 0.05% antifoam, and administered orally to mice (12.5 mg/kg twice daily). EOMA cells (0.3×106) are injected subcutaneously in 6- to 8-week-old nu/nu female mice (2 sites/mouse, 4-5 mice/group). Tumor size is measured daily. For drug treatment, when tumors reach 0.01 cm3 in size, the animals are treated with vehicle control or LY-2584702 (12.5 mg/kg twice daily, oral dosing). Tumor size is measured every 3 to 4 days[2].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献

  • [1]. Tolcher A, et al. A phase I trial of LY2584702 tosylate, a p70 S6 kinase inhibitor, in patients with advanced solid tumors. Eur J Cancer. 2014 Mar;50(5):867-75.

    [2]. Phung TL, et al. Akt1 and akt3 exert opposing roles in the regulation of vascular tumor growth. Cancer Res. 2015 Jan 1;75(1):40-50.

    [3]. Chen B, et al. Hyperphosphorylation of RPS6KB1, rather than overexpression, predicts worse prognosis in non-small cell lung cancer patients. PLoS One. 2017 Aug 9;12(8):e0182891.

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

Genz-123346 free base

发表于由

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。

Genz-123346 free base  纯度: 99.82%

Genz-123346是阻断神经酰胺向GL1转化的GL1合酶的抑制剂；抑制GM1IC50值为14 nM。

Genz-123346 free base

Genz-123346 free base Chemical Structure

CAS No. : 491833-30-8

规格 价格 是否有货 数量
Free Sample (0.1-0.5 mg)   Apply now  
10 mM * 1 mL in DMSO ￥1815 In-stock
5 mg ￥1650 In-stock
10 mg ￥2700 In-stock
25 mg ￥5400 In-stock
50 mg ￥8600 In-stock
100 mg   询价  
200 mg   询价  

* Please select Quantity before adding items.

Genz-123346 free base 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus
  • Anti-Cancer Compound Library
  • Diabetes Related Compound Library
  • Targeted Diversity Library

生物活性

Genz-123346 (free base) is an inhibitor of GL1 synthase that blocks the conversion of ceramide to GL1; inhibits GM1 with IC50 value of 14 nM.

IC50 & Target

IC50: 14 nM (GM1)[1]
体外研究
(In Vitro)

Exposure of cells to Genz-123346 and to other GCS inhibitors at nontoxic concentrations can enhance the killing of tumor cells by cytotoxic anti-cancer agents. Genz-123346 and a few other GCS inhibitors are substrates for multi-drug resistance efflux pumps such as P-gp (ABCB1, gP-170). In cell lines selected to over-express P-gp or which endogenously express P-gp, chemosensitization by Genz-123346 is primarily due to the effects on P-gp function[2]. Genz-123346(Genz) is an enhancer of autophagy flux[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)

In the Zucker diabetic fatty rat, Genz-123346 loared glucose and A1C levels and improved glucose tolerance. Drug treatment also prevented the loss of pancreatic beta-cell function and preserved the ability of the animals to secrete insulin. In the diet-induced obese mouse, treatment with Genz-123346 normalized A1C levels and improved glucose tolerance. The oral bioavailability of the drug is shown to be about 10% and 30% in mice and rats, respectively, with a half-life in plasma of 30–60 min[1]. Genz-123346 treatment results in a dose-dependent reduction of renal GlcCer and GM3 levels that translates into effective inhibition of cystic disease. A direct effect of Genz-123346 on the Akt-mTOR signaling pathway is observed, with reduced phosphorylation of Akt and ribosomal protein S6[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

418.57

Formula

C24H38N2O4
CAS 号

491833-30-8
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 (238.91 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 2.3891 mL 11.9454 mL 23.8909 mL
5 mM 0.4778 mL 2.3891 mL 4.7782 mL
10 mM 0.2389 mL 1.1945 mL 2.3891 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: ≥ 3 mg/mL (7.17 mM); Clear solution

    此方案可获得 ≥ 3 mg/mL (7.17 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 30.0 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: ≥ 3 mg/mL (7.17 mM); Clear solution

    此方案可获得 ≥ 3 mg/mL (7.17 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 30.0 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: ≥ 3 mg/mL (7.17 mM); Clear solution

    此方案可获得 ≥ 3 mg/mL (7.17 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 30.0 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]. Zhao H, et al. Inhibiting glycosphingolipid synthesis improves glycemic control and insulin sensitivity in animal models of type 2 diabetes. Diabetes. 2007 May;56(5):1210-8.

    [2]. Chai L, et al. The chemosensitizing activity of inhibitors of glucosylceramide synthase is mediated primarily through modulation of P-gp function. Int J Oncol. 2011 Mar;38(3):701-11.

    [3]. Shen W, et al. Inhibition of glucosylceramide synthase stimulates autophagy flux in neurons. J Neurochem. 2014 Jun;129(5):884-94

    [4]. Natoli TA, et al. Inhibition of glucosylceramide accumulation results in effective blockade of polycystic kidney disease in mouse models. Nat Med. 2010 Jul;16(7):788-92.
Animal Administration
[1]

Rats: Genz-123346 is dissolved in water. Zucker diabetic fatty rats treated with Genz-123346 (75 mg/kg) for 6 weeks are fasted overnight. The following morning, the fasted rats are anesthetized and injected with 5 units human insulin into the hepatic portal vein. Quadriceps muscle and liver are harvested 2 min after injection and immediately frozen in liquid nitrogen. Insulin receptor is immunoprecipitated. The immunoprecipitates are analyzed by immunoblotting[1].

Mice: C57BL/6 mice are fed on a high-fat (45% of kcal) diet for 8 weeks, obese mice with comparable body weight gain, glucose, and insulin levels are assigned to either the treated or control groups. The mice are then gavaged daily with Genz-123346 or water for 10 weeks[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.
参考文献

  • [1]. Zhao H, et al. Inhibiting glycosphingolipid synthesis improves glycemic control and insulin sensitivity in animal models of type 2 diabetes. Diabetes. 2007 May;56(5):1210-8.

    [2]. Chai L, et al. The chemosensitizing activity of inhibitors of glucosylceramide synthase is mediated primarily through modulation of P-gp function. Int J Oncol. 2011 Mar;38(3):701-11.

    [3]. Shen W, et al. Inhibition of glucosylceramide synthase stimulates autophagy flux in neurons. J Neurochem. 2014 Jun;129(5):884-94

    [4]. Natoli TA, et al. Inhibition of glucosylceramide accumulation results in effective blockade of polycystic kidney disease in mouse models. Nat Med. 2010 Jul;16(7):788-92.

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

Taletrectinib free base(Synonyms: DS-6051b free base; AB-106 free base)

发表于由

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。

Taletrectinib free base (Synonyms: DS-6051b free base; AB-106 free base)

Taletrectinib (DS-6051b) free base 是一种有效的口服活性下一代选择性 ROS1/NTRK 抑制剂。Taletrectinib free base 分别以0.207、0.622、2.28 和 0.98 nM 的 IC50 对重组 ROS1、NTRK1、NTRK2 和 NTRK3 有较强的抑制作用。Taletrectinib free base还抑制 ROS1 G2032R 和其他抗 Crizotinib 的 ROS1 突变体。

Taletrectinib free base(Synonyms: DS-6051b free base; AB-106 free base)

Taletrectinib free base Chemical Structure

CAS No. : 1505514-27-1

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Taletrectinib free base 的其他形式现货产品:

Taletrectinib

生物活性

Taletrectinib (DS-6051b) free base is a potent, orally active, and next-generation selective ROS1/NTRK inhibitor. Taletrectinib free base potently inhibits recombinant ROS1, NTRK1, NTRK2, and NTRK3 with IC50s of 0.207, 0.622, 2.28, and 0.98 nM, respectively. Taletrectinib free base also inhibits ROS1 G2032R and other Crizotinib-resistant ROS1 mutants[1][2].

体外研究
(In Vitro)

The IC50 of Taletrectinib free base (1-1000 nM; 72 hours) against Ba/F3-TPM3-NTRK1, Ba/F3-ETV6-NTRK1, -NTRK2, -NTRK3, or KM12 cells is ~3-20 nM[1].
Taletrectinib free base (0.001-1000 nM; 2 hours) dose dependently inhibited autophosphorylation of ROS1 in U-118-MG cells in vitro[1].
Taletrectinib (DS-6051b) free base potently inhibits autophosphorylation of ROS1 in JFCR-165, JFCR-168, and MGH193-1B cells[1].
Taletrectinib free base partially suppresses phospho-NTRK1 at 10 nM, and completely suppresses by 100 nM. Taletrectinib free base potently inhibits recombinant ROS1, NTRK1, and NTRK3 in sub-nanomolar concentration in an ATP-competitive manner. Taletrectinib free base almost completely inhibits ACK, ALK, DDR1, and LTK at 0.2 μM among 160 kinases in the presence of 1 mM ATP, but did not inhibit other 152 kinases strongly[1].
Taletrectinib free base effectively inhibits Crizotinib-resistant ROS1 secondary mutations, including G2032R solvent front mutation[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[1]

Cell Line: TPM3-NTRK1-induced Ba/F3 cells, KM12 cells
Concentration: 1-1000 nM
Incubation Time: 72 hours
Result: Inhibited TPM3-NTRK1-induced Ba/F3 cells and KM12 cells viability.

Western Blot Analysis[1]

Cell Line: U-118 MG cells (harboring FIG-ROS1 fusion gene)
Concentration: 0.001-1000 nM
Incubation Time: 2 hours
Result: Dose dependently inhibited autophosphorylation of ROS1 in U-118-MG cells.

体内研究
(In Vivo)

Taletrectinib (DS-6051b) free base (25-200 mg/kg; p.o.; once daily for 18 days) shows antitumor activity[1].
Taletrectinib free base (6.25-200 mg/kg; p.o.; once daily for 8 days) inhibits NTRK-rearranged cancer in Balb-c nu/nu mice bearing KM12 cells[1].
Taletrectinib free base (3-100 mg/kg; p.o.; once daily for 4 days) shows rapid tumor regression in the wild-type (WT) and the G2032R-mutant Ba/F3-bearing mice without severe body weight loss[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Balb-c nu/nu mice (bearing U-118 MG cells)[1]
Dosage: 25, 50, 100, and 200 mg/kg
Administration: P.o.; once daily for 18 days
Result: Effectively inhibited tumor growth at ≥25 mg/kg without significant body weight loss.

Clinical Trial

分子量

405.47

Formula

C23H24FN5O
CAS 号

1505514-27-1
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]. Katayama R, et al. The new-generation selective ROS1/NTRK inhibitor DS-6051b overcomes crizotinib resistant ROS1-G2032R mutation in preclinical models. Nat Commun. 2019;10(1):3604. Published 2019 Aug 9.

    [2]. Fujiwara Y, et al. Safety and pharmacokinetics of DS-6051b in Japanese patients with non-small cell lung cancer harboring ROS1 fusions: a phase I study. Oncotarget. 2018;9(34):23729-23737. Published 2018 May 4.

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SR-717 free acid

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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。

SR-717 free acid 

SR-717 free acid 是一种非核苷类 STING 激动剂，在 ISG-THP1 (WT) 和 ISG-THP1 cGAS KO (cGAS KO) 细胞中的 EC50 分别为 2.1 μM 和 2.2 μM。SR-717 free acid 是一种稳定的环鸟苷单磷酸腺苷单磷酸 (cGAMP) 类似物。具有抗肿瘤活性。

SR-717 free acid

SR-717 free acid Chemical Structure

CAS No. : 2375420-34-9

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SR-717 free acid 的其他形式现货产品:

SR-717

生物活性

SR-717 free acid is a non-nucleotide STING agonist with EC50s of 2.1 μM and 2.2 μM in ISG-THP1 (WT) and ISG-THP1 cGAS KO (cGAS KO) cell lines, respectively. SR-717 free acid is a stable cyclic guanosine monophosphate-adenosine monophosphate (cGAMP) mimetic. Antitumor activity[1].

体外研究
(In Vitro)

SR-717 activates STING by inducing the same closed conformation, which thereby provides an avenue to explore this class of systemic STING agonist in diverse contexts, including antitumor immunity[1].
SR-717 (3.8 μM) induces the expression of PD-L1 in THP1 cells and in primary human peripheral blood mononuclear cells in a STING-dependent manner[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究
(In Vivo)

SR-717 (30 mg/kg intraperitoneal once-per-day for 1 week) shows antitumor activities in WT or Stinggt/gt mice[1].
SR-717 (30 mg/kg intraperitoneally for 7 days) displays antitumor activity; promots the activation of CD8+ T, natural killer, and dendritic cells in relevant tissues; and facilitates antigen cross-priming[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: WT or Stinggt/gt mice[1]
Dosage: 30 mg/kg
Administration: Intraperitoneally; once-per-day for 1 week
Result: Maximally inhibited tumor growth.

分子量

345.26

Formula

C15H9F2N5O3
CAS 号

2375420-34-9
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]. Emily N Chin, et al. Antitumor activity of a systemic STING-activating non-nucleotide cGAMP mimetic. Science. 2020 Aug 21;369(6506):993-999.

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多肽定制[Arg8]-Vasopressin (free acid) net 编码 [25255-33-8]

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名称 [Arg8]-Vasopressin (free acid) net
编码 [25255-33-8]
别名 [Arg8]-Vasopressin (free acid) net
纯度 80%，90%，95%，98%，99%
重量 1mg,5mg,10mg,50mg,100mg,1g
序列（单字母缩写） CYFQNCPRG[Cys1-Cys6 bridge]
序列（三字母缩写） Cys-Tyr-Phe-Gln-Asn-Cys-Pro-Arg-Gly(Cys1-Cys6 bridge)
基本描述
溶解度
分子量 1085.24
化学式 C46H64N14O13S2
存储条件 Store at -20°C. Keep tightly closed. Store in a cool dry place.
注释
Documents [Arg8]-Vasopressin (free acid) net 编码 [25255-33-8]
Figures [Arg8]-Vasopressin (free acid) net 编码 [25255-33-8]
Reference
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化学桥 (Cys1-Cys6 bridge)

(Arg8)-Vasopressin (free acid) 编码 [25255-33-8]

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名称 (Arg8)-Vasopressin (free acid)
编码 [25255-33-8]
别名 (Arg8)-Vasopressin (free acid)
纯度 80%，90%，95%，98%，99%
重量 1mg,5mg,10mg,50mg,100mg,1g
序列（单字母缩写） CYFQNCPRG-OH
序列（三字母缩写） Cys-Tyr-Phe-Gln-Asn-Cys-Pro-Arg-Gly
基本描述
溶解度
分子量 0
化学式
存储条件 Store at -20°C. Keep tightly closed. Store in a cool dry place.
注释
Documents (Arg8)-Vasopressin (free acid) 编码 [25255-33-8]
Figures (Arg8)-Vasopressin (free acid) 编码 [25255-33-8]
Reference
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N端
化学桥

多肽定制[Lys8]-Vasotocin (free acid) 编码

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上海金畔生物科技有限公司可以定制不同序列多肽，可以访问官网了解更多产品信息。

名称 [Lys8]-Vasotocin (free acid)
编码
别名 [Lys8]-Vasotocin (free acid)
纯度 80%，90%，95%，98%，99%
重量 1mg,5mg,10mg,50mg,100mg,1g
序列（单字母缩写） CYIQNCPKG[Cys1-Cys6 bridge]
序列（三字母缩写） Cys-Tyr-Ile-Gln-Asn-Cys-Pro-Lys-Gly(Cys1-Cys6 bridge)
基本描述
溶解度
分子量 1023.21
化学式 C43H66N12O13S2
存储条件 Store at -20°C. Keep tightly closed. Store in a cool dry place.
注释
Documents [Lys8]-Vasotocin (free acid) 编码
Figures [Lys8]-Vasotocin (free acid) 编码
Reference
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化学桥 (Cys1-Cys6 bridge)

WS-383 free base

发表于由

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。

WS-383 free base 

WS-383 free base 是一种有效、选择性、可逆的 DCN1-UBC12 相互作用抑制剂，IC50 值为 11 nM。WS-383 free base 抑制 Cul3/1 的类泛素化修饰，引起 p21，p27 和 NRF2 的积累。

WS-383 free base

WS-383 free base Chemical Structure

CAS No. : 2247543-65-1

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WS-383 free base 的其他形式现货产品:

WS-383

生物活性

WS-383 free base is a potent, selective and reversible inhibitor of DCN1-UBC12 interaction, with an IC50 of 11 nM. WS-383 free base inhibits Cul3/1 neddylation, induces accumulation of p21, p27 and NRF2[1].

IC50 & Target

IC50: 11 nM (DCN1–UBC12 interaction)[1]
体外研究
(In Vitro)

WS-383 (10 μM) is against a panel of kinases such as BTK, CDKs, and EGFR [L858R] using staurosporine and afatinib as the positive controls. WS-383 showed weak inhibitory activity at 10.0 μM,it is selective to the DCN1–UBC12 interaction over the selected kinasesr[1].
WS-383 (0.03-3 μM;24 hours) blocks Cul3 neddylation at 3 μM and also has certain inhibition of Cul1 neddylation at 10 μM but was not effective in inhibiting neddylation of other cullin members[1].
WS-383 (0.03-3 μM;24 hours) increases Cul1, Skp1 (adaptor protein), F-box protein, and RBX1/RBX2 RING protein form SCF E3 complex. Cyclin dependent kinase inhibitor 1A (p21) and cyclin dependent kinase inhibitor 1B (p27) expression in a dose-dependent manner in MGC-803 and KYSE70 manner[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis[1]

Cell Line: MGC-803 cells
Concentration: 0.03 μM; 0.3 μM; 3 μM; 10 μM
Incubation Time: 24 hours
Result: Decreased N8-Cul1 and N8-Cul2 protein expression.

Western Blot Analysis[1]

Cell Line: MGC-803 and KYSE70 cells
Concentration: 0.03 μM; 0.3 μM; 3 μM; 10 μM
Incubation Time: 24 hours
Result: Induced accumulation of p21, p27, and NRF2 in MGC-803 cells.

分子量

461.99

Formula

C18H20ClN9S2
CAS 号

2247543-65-1
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]. Wang S, et al. Development of Highly Potent, Selective, and Cellular Active Triazolo[1,5- a]pyrimidine-Based Inhibitors Targeting the DCN1-UBC12 Protein-Protein Interaction.J Med Chem. 2019 Mar 14;62(5):2772-2797.

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多肽定制Allatostatin I (free acid) 编码

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上海金畔生物科技有限公司可以定制不同序列多肽，可以访问官网了解更多产品信息。

名称 Allatostatin I (free acid)
编码
别名 Allatostatin I (free acid)
纯度 80%，90%，95%，98%，99%
重量 1mg,5mg,10mg,50mg,100mg,1g
序列（单字母缩写） APSGAQRLYGFGL
序列（三字母缩写） Ala-Pro-Ser-Gly-Ala-Gln-Arg-Leu-Tyr-Gly-Phe-Gly-Leu
基本描述
溶解度
分子量 1336.54
化学式 C61H93N17O17
存储条件 Store at -20°C. Keep tightly closed. Store in a cool dry place.
注释
Documents Allatostatin I (free acid) 编码
Figures Allatostatin I (free acid) 编码
Reference
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化学桥

JNJ-63576253 free base(Synonyms: TRC-253 free base)

发表于由

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。

JNJ-63576253 free base (Synonyms: TRC-253 free base)

JNJ-63576253 (TRC-253) free base 是一种有效和具有口服活性的雄激素受体 (androgen receptor) 的完全拮抗剂，在 LNCaP 细胞中对 F877L 突变型 AR 和野生型 AR 的 IC50 值分别为 37 和 54 nM。JNJ-63576253 free base 可用于去势抵抗性前列腺癌 (CRPC) 的研究。

JNJ-63576253 free base(Synonyms: TRC-253 free base)

JNJ-63576253 free base Chemical Structure

CAS No. : 2110426-27-0

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JNJ-63576253 free base 的其他形式现货产品:

JNJ-63576253

生物活性

JNJ-63576253 (TRC-253) free base is a potent and orally active full antagonist of androgen receptor (AR), with IC50s of 37 and 54 nM for F877L mutant AR and wild-type AR in LNCaP cells. JNJ-63576253 free base can be used for the research of castration-resistant prostate cancer (CRPC)[1].

IC50 & Target

IC50: 37 nM (F877L mutant AR in LNCaP cells); 54 nM (wild-type AR in LNCaP cells)[1]
体外研究
(In Vitro)

JNJ-63576253 (0.0003-100 μM; 5 d) inhibits the growth of VCaP cells, with an IC50 of 265 nM[1].
JNJ-63576253 is stable in human liver microsomes, with an T1/2 of >180 min[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究
(In Vivo)

JNJ-63576253 (30 mg/kg; p.o. once daily for 72 days) significantly inhibits the growth of prostate LNCaP SRα F877L tumor in mice[1].
JNJ-63576253 (30 mg/kg; p.o. once daily for 10 days) inhibits the five androgen sensitive organs (ASOs) under stimulation by testosterone propionate (TP) in mice[1].
JNJ-63576253 (10 mg/kg; p.o.) exhibits moderate oral bioavailability (45%), Cmax (0.66 μM) and AUClast (4.9 μg•h/mL) in mice[1].
JNJ-63576253 (2 mg/kg; i.v.) exhibits reasonable half-life (5.99 h), CL (15.0 mL/min/kg) and Vdss (6.11 L/kg) in mice[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Castrated SHO mice with prostate LNCaP SRα F877L tumor[1]
Dosage: 30 mg/kg
Administration: P.o. once daily for 72 days
Result: Inhibited the tumor growth by 87%.
Animal Model: CD-1 male mice[1]
Dosage: 2 mg/kg for i.v.; 10 mg/kg for p.o. (Pharmacokinetic Analysis)
Administration: Intravenous administration and oral administration
Result: I.v.: T1/2=5.99 h; CL=15.0 mL/min/kg; Vdss=6.11 L/kg.
P.o.: F=45%; Cmax=0.66 μM; AUClast=4.9 μg•h/mL.

Clinical Trial

分子量

502.51

Formula

C23H21F3N6O2S
CAS 号

2110426-27-0
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]. Zhang Z, et, al. Discovery of JNJ-63576253: A Clinical Stage Androgen Receptor Antagonist for F877L Mutant and Wild-Type Castration-Resistant Prostate Cancer (mCRPC). J Med Chem. 2021 Jan 28;64(2):909-924.

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Hu7691 free base

发表于由

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。

Hu7691 free base 

Hu7691 free base 是一种具有口服活性的，选择性 Akt 抑制剂，对 Akt1、Akt2 和 Akt3 的 IC50 分别为 4.0 nM、97.5 nM、28 nM。Hu7691 free base 抑制肿瘤生长并降低小鼠的皮肤毒性。

Hu7691 free base

Hu7691 free base Chemical Structure

CAS No. : 2241232-43-7

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生物活性

Hu7691 free base is an orally active, selective Akt inhibitor with IC50s of 4.0 nM, 97.5 nM, 28 nM for Akt1, Akt2 and Akt3, respectively. Hu7691 free base inhibits tumor growth and enables decrease of cutaneous toxicity in mice[1].

IC50 & Target[1]

Akt1

4.0 nM (IC50)

Akt2

97.5 nM (IC50)

Akt3

28 nM (IC50)

PKA

11 nM (IC50)

PKCη

629 nM (IC50)

ROCK1

354 nM (IC50)

RSK1

756 nM (IC50)

p70S6K

229 nM (IC50)

体外研究
(In Vitro)

Hu7691 free base displays low inhibitions against most of the kinases in the four families (AGC, TK, TKL, Lipid/Atypical; PKA, IC50=11 nM; PKCη, IC50=629 nM; ROCK1, IC50=354 nM; RSK1, IC50=756 nM; P70S6K, IC50=229 nM; SGK, IC50=1009 nM)[1].
Hu7691 free base (2.25-36 μM; 24 hours) induces effective decrease of the phosphorylation level of Akt (S473)[1].
Hu7691 free base (10, 20, 30, 40 μM; for 72 h) exhibits low toxicity against HaCaT cells with an IC50 value of 15.2 μM[1].
Hu7691 free base has a significant inhibitory effect on the growth of 18 kinds of human tumor cells (U87-MG, U251, A549, HepG2, HT-29, KHOS, MDA-MB-231, PC3, SKOV3 and so on) derived from different tissues, with the IC50 range of 0.6-27 μM. Hu7691 free base shows low antiproliferation activities against the HL7702 and HPDE6-C7 normal cells, exhibiting IC50 values of 5.4 and 16.1 μM, respectively[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis[1]

Cell Line: HaCaT cells
Concentration: 2.25, 4.5, 9, 18, 36 μM
Incubation Time: 24 hours
Result: Induced effective decrease of the phosphorylation level of Akt (S473).

体内研究
(In Vivo)

Hu7691 free base (12.5-50 mg/kg/day; i.g.; for 22 days) shows dose-dependent tumor growth inhibition[1].
Hu7691 free base (15 mg/kg; oral) has a T1/2 of 8.68 hours, a Cmax of 171.17 ng/mL and an AUC of 2820.64 ng/mL•h in rats[1].
Hu7691 free base (2 mg/kg; iv) has a T1/2 of 6.24 hours, a Cmax of 207.52 ng/mL and an AUC of 532.87 ng/mL•h in rats[1].
Hu7691 free base (20 mg/kg; oral) has a T1/2 of 16.7 hours, a Cmax of 905.65 ng/mL and an AUC of 36303 ng/mL•h in beagle dog (male, 40 weeks old, 8–10 kg)[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Balb/c mice (nu/nu, female, 3-4 weeks old, 20-25 g) with 786-O and KHOS xenograft[1]
Dosage: 12.5, 25, 50 mg/kg
Administration: Oral; once daily for 22 days
Result: Showed dose-dependent tumor growth inhibition.
Animal Model: SD rats (male, 8 weeks old, 250-300 g)[1]
Dosage: 15 mg/kg (Pharmacokinetic Analysis)
Administration: Oral
Result: Had a T1/2 of 8.68 hours, a Cmax of 171.17 ng/mL and an AUC of 2820.64 ng/mL•h.

分子量

414.42

Formula

C22H21F3N4O
CAS 号

2241232-43-7
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]. Jinxin Che, et al. Discovery of N-((3 S,4 S)-4-(3,4-Difluorophenyl)piperidin-3-yl)-2-fluoro-4-(1-methyl-1 H-pyrazol-5-yl)benzamide (Hu7691), a Potent and Selective Akt Inhibitor That Enables Decrease of Cutaneous Toxicity. J Med Chem. 2021 Aug 26;64(16):12163-12180.

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Tamsulosin(Synonyms: 坦索罗辛; (R)-(-)-YM12617 free base; LY253351 free base)

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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。

Tamsulosin (Synonyms: 坦索罗辛; (R)-(-)-YM12617 free base; LY253351 free base) 纯度: 99.62%

Tamsulosin ((R)-(-)-YM12617 free base) 是一种 α1 肾上腺素能受体 (α1-adrenergic receptor) 抑制剂。Tamsulosin 常用于前列腺增生的研究。在动物模型中，Tamsulosin 可减缓腹主动脉瘤的生长。

Tamsulosin(Synonyms: 坦索罗辛; (R)-(-)-YM12617 free base; LY253351 free base)

Tamsulosin Chemical Structure

CAS No. : 106133-20-4

规格 价格 是否有货 数量
Free Sample (0.1-0.5 mg)   Apply now  
10 mM * 1 mL in DMSO ￥660 In-stock
10 mg ￥550 In-stock
50 mg ￥1350 In-stock
100 mg ￥2250 In-stock
200 mg   询价  
500 mg   询价  

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生物活性

Tamsulosin ((R)-(-)-YM12617 free base) is an inhibitor of α1-adrenergic receptor. Tamsulosin is used for the research of prostatic hyperplasia. Tamsulosin attenuates abdominal aortic aneurysm growth in animal models[1].

IC50 & Target[1]

α1-adrenergic receptor

 

Clinical Trial

分子量

408.51

Formula

C20H28N2O5S
CAS 号

106133-20-4
中文名称

坦索罗辛；坦洛新；坦索洛新
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 (244.79 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.4479 mL 12.2396 mL 24.4792 mL
5 mM 0.4896 mL 2.4479 mL 4.8958 mL
10 mM 0.2448 mL 1.2240 mL 2.4479 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 (6.12 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (6.12 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 (6.12 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (6.12 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 (6.12 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (6.12 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]. Christopher Chapple, et al. Tamsulosin: an overview. World J Urol. 2002 Apr;19(6):397-404.

    [2]. William G. Montgomery, BA, et al. Tamsulosin Attenuates Abdominal Aortic Aneurysm Growth. Surgery. 2018 Nov; 164(5): 1087–1092.

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MA242 free base

发表于由

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。

MA242 free base 

MA242 free base 是特异性的 MDM2 和 NFAT1 双重抑制剂。MA242 free base 以高亲和力直接结合 MDM2 和 NFAT1，诱导 MDM2 和 NFAT1 蛋白降解，并抑制 NFAT1 介导的 MDM2 转录。MA242 free base 在胰腺癌细胞系中诱导凋亡。

MA242 free base

MA242 free base Chemical Structure

CAS No. : 1049704-17-7

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

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生物活性

MA242 free base is a specific dual inhibitor of MDM2 and NFAT1. MA242 free base directly binds both MDM2 and NFAT1 with high affinity, induces their protein degradation, and inhibits NFAT1-mediated transcription of MDM2. MA242 free base induces apoptosis in pancreatic cancer cell lines regardless of p53 status[1].

IC50 & Target

MDM2, NFAT1[1]
体外研究
(In Vitro)

MA242 (0.05-5 μM; 72 hours) free base significantly inhibits pancreatic cancer cell growth, with IC50s ranging from 0.1 to 0.4 μM, regardless of the p53 status of the cells. However, MA242 free base shows minimal effects on the growth of normal HPDE cells (IC50=5.81 μM), indicating that MA242 has selective effects against cancer cells[1].
MA242 (0.1-0.5 μM; 24 hours) free base significantly decreases the MDM2 and NFAT1 protein levels at a low concentration in all three cell lines[1].
MA242 free base decreases cell proliferation and induces apoptosis in pancreatic cancer cell lines regardless of p53 status[1].
MA242 free base alone or in combination with Gemcitabine inhibits pancreatic tumor growth and metastasis without any host toxicity[1].
MA242 free base exerts cytotoxicity against hepatocellular carcinoma (HCC) cells by inhibiting the NFAT1-MDM2 pathway in vitro, independent of p53. MA242 showed selective cytotoxicity against HCC cells, with IC50 values ranging from 0.1-0.31 μM[2].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[1]

Cell Line: The human pancreatic cancer HPAC, Panc-1, AsPC-1, Mia-Paca-2 and BxPC-3 cell lines; The human pancreatic ductal epithelium (HPDE) cell line
Concentration: 0.05, 0.5, and 5 μM
Incubation Time: 72 hours
Result: The IC50s are 0.14, 0.14, 0.15, 0.25, 0.40, and 5.81 μM for Panc-1, Mia-Paca-2, AsPC-1, BxPC-3, HPAC, and HPDE cells, respectively.

Western Blot Analysis[1]

Cell Line: The human pancreatic cancer HPAC, Panc-1, and AsPC-1 cell lines
Concentration: 0, 0.1, 0.2, and 0.5 μM
Incubation Time: 24 hours
Result: Decreased the expression of MDM2 and NFAT1.

体内研究
(In Vivo)

MA242 (IP; 2.5, 5, 10 mg/kg) free base suppresses orthotopic pancreatic tumor growth in vivo, independent of p53[1].
There were no significant differences in the average body weights between the vehicle- and MA242 free base-treated mice in either of the models, did not have significant host toxicity at these effective doses[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Female 4-6-week-old athymic nude mice (nu/nu, 4-6 weeks) bearing AsPC-1-Luc or Panc-1-Luc tumor[1]
Dosage: 2.5 or 5 mg/kg for Panc-1 tumor-bearing mice; 10 mg/kg for AsPC-1 tumor-bearing mice
Administration: IP; 2.5 or 5 mg/kg/d, 5 d/wk for five weeks for Panc-1 tumor-bearing mice;
IP; 10 mg/kg/d, 5 d/wk for three weeks for AsPC-1 tumor-bearing mice
Result: Resulted in 56.1% and 82.5% inhibition of tumor growth in nude mice bearing Panc-1 orthotopic tumors, respectively.
Significantly suppressed the growth of AsPC-1 orthotopic tumors by 89.5% (P < 0.01) compared with the tumors in control animals.
Led to almost complete tumor regression in MD242-treated mice in both models.

分子量

465.95

Formula

C24H20ClN3O3S
CAS 号

1049704-17-7
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]. Wei Wang, et al. Discovery and Characterization of Dual Inhibitors of MDM2 and NFAT1 for Pancreatic Cancer Therapy. Cancer Res. 2018 Oct 1;78(19):5656-5667.

    [2]. Wei Wang, et al. MDM2-NFAT1 dual inhibitor, MA242: Effective against hepatocellular carcinoma, independent of p53. Cancer Lett. 2019 Sep 10;459:156-167.

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多肽定制Cecropin B, Free Acid 编码

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上海金畔生物科技有限公司可以定制不同序列多肽，可以访问官网了解更多产品信息。

名称 Cecropin B, Free Acid
编码
别名 Cecropin B, Free Acid
纯度 80%，90%，95%，98%，99%
重量 1mg,5mg,10mg,50mg,100mg,1g
序列（单字母缩写） KWKVFKKIEKMGRNIRNGIVKAGPAIAVLGEAKAL
序列（三字母缩写） Lys-Trp-Lys-Val-Phe-Lys-Lys-Ile-Glu-Lys-Met-Gly-Arg-Asn-Ile-Arg-Asn-Gly-Ile-Val-Lys-Ala-Gly-Pro-Ala-Ile-Ala-Val-Leu-Gly-Glu-Ala-Lys-Ala-Leu
基本描述
溶解度
分子量 3835.92
化学式 C176H301N51O42S
存储条件 Store at -20°C. Keep tightly closed. Store in a cool dry place.
注释
Documents Cecropin B, Free Acid 编码
Figures Cecropin B, Free Acid 编码
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多肽定制Chlorotoxin (free acid) 编码

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上海金畔生物科技有限公司可以定制不同序列多肽，可以访问官网了解更多产品信息。

名称 Chlorotoxin (free acid)
编码
别名 Chlorotoxin (free acid)
纯度 80%，90%，95%，98%，99%
重量 1mg,5mg,10mg,50mg,100mg,1g
序列（单字母缩写） MCMPCFTTDHQMARKCDDCCGGKGRGKCYGPQCLCR-OH
序列（三字母缩写） Met-Cys-Met-Pro-Cys-Phe-Thr-Thr-Asp-His-Gln-Met-Ala-Arg-Lys-Cys-Asp-Asp-Cys-Cys-Gly-Gly-Lys-Gly-Arg-Gly-Lys-Cys-Tyr-Gly-Pro-Gln-Cys-Leu-Cys-Arg
基本描述
溶解度
分子量 0
化学式
存储条件 Store at -20°C. Keep tightly closed. Store in a cool dry place.
注释
Documents Chlorotoxin (free acid) 编码
Figures Chlorotoxin (free acid) 编码
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多肽定制Cholecystokinin Octapeptide free acid (desulfated) 编码 [103974-46-5]

发表于由

上海金畔生物科技有限公司可以定制不同序列多肽，可以访问官网了解更多产品信息。

名称 Cholecystokinin Octapeptide free acid (desulfated)
编码 [103974-46-5]
别名 Cholecystokinin Octapeptide free acid (desulfated)
纯度 80%，90%，95%，98%，99%
重量 1mg,5mg,10mg,50mg,100mg,1g
序列（单字母缩写） DYMGWMDF
序列（三字母缩写） Asp-Tyr-Met-Gly-Trp-Met-Asp-Phe
基本描述
溶解度
分子量 1064.21
化学式 C49H61N9O13S2
存储条件 Store at -20°C. Keep tightly closed. Store in a cool dry place.
注释
Documents Cholecystokinin Octapeptide free acid (desulfated) 编码 [103974-46-5]
Figures Cholecystokinin Octapeptide free acid (desulfated) 编码 [103974-46-5]
Reference
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