标签归档：sb

SB-505124 hydrochloride

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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。

SB-505124 hydrochloride 

SB-505124 hydrochloride 是一种选择性的 TGF-β Receptor type I receptor (ALK4，ALK5，ALK7) 抑制剂，对 LK4，ALK5 的 IC50 值分别为 129 nM 和 47 nM，对 ALK1，2，3 或 6 无作用。

SB-505124 hydrochloride

SB-505124 hydrochloride Chemical Structure

CAS No. : 356559-13-2

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SB-505124 hydrochloride 的其他形式现货产品:

SB-505124

生物活性

SB-505124 hydrochloride is a selective inhibitor of TGF-β Receptor type I receptor (ALK4, ALK5, ALK7), with IC50s of 129 nM and 47 nM for ALK4, ALK5, respectively, but it does not inhibit ALK1, 2, 3, or 6.

IC50 & Target

IC50: 129 nM (ALK4), 47 nM (ALK5)
体外研究
(In Vitro)

SB-505124 demonstrates no toxicity to renal epithelial A498 cells at concentrations up to 100 μM for 48 h. 505124 inhibits the closely related ALK4 with an IC50 value of 129±11 nM (about 2.5-fold less sensitive than ALK5) but does not inhibit ALK2 at concentrations up to 10 μM. SB-505124 (1 μM) inhibits the TGF-β-induced phosphorylation of Smad2 in all three of these cell lines in a concentration-dependent fashion. SB-505124 (1 or 5 μM) potently inhibits TGF-β-induced activation of JNK/SAP, extracellular signal-regulated kinase 1/2, and p38 despite the different patterns of activation in these cells[1]. SB-505124 (10 µM) impairs Smad2 phosphorylation and CTGF and α-SMA expression in vitro[2]. SB-505124 susspresses CTGF and α-SMA observed by immunofluorescence. Cell outgrowth from explants dissected from eyes to which SB-505124 is applied during GFS is robust while outgrowth is poor from those treated with MMC[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)

SB-505124 (5 mg/kg; i.p.) alone has no effect in C57Bl6 mice with A549 xenografts, but administration of SB-505124 with a single dose of Carboplatin (60 mg/kg) results in durable responses without the need for maintenance therapy in five animals[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.

Animal Model: C57Bl6 mice with A549 xenografts[4]
Dosage: 5 mg/kg
Administration: I.p.; daily
Result: Had no effect alone, but administration with a single dose of carboplatin (60 mg/kg) resulted in durable responses without the need for maintenance therapy in five animals.

分子量

371.86

Formula

C20H22ClN3O2
CAS 号

356559-13-2
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]. DaCosta Byfield S, et al. SB-505124 is a selective inhibitor of transforming growth factor-beta type I receptors ALK4, ALK5, and ALK7. Mol Pharmacol. 2004 Mar;65(3):744-52.

    [2]. Sutariya V, et al. reversible gel for delivery of receptor-like kinase 5 inhibitor SB-505124 for glaucoma filtration surgery. Pharm Dev Technol. 2013 Jul-Aug;18(4):957-62.

    [3]. Sapitro J, et al. Suppression of transforming growth factor-β effects in rabbit subconjunctival fibroblasts by receptor-like kinase 5 inhibitor. Mol Vis. 2010 Sep 16;16:1880-92.

    [4]. Marini KD, et al. Inhibition of activin signaling in lung adenocarcinoma increases the therapeutic index of platinum chemotherapy. Sci Transl Med. 2018 Jul 25;10(451). pii: eaat3504.

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Adezmapimod(Synonyms: SB 203580; RWJ 64809)

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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。

Adezmapimod (Synonyms: SB 203580; RWJ 64809) 纯度: 99.86%

Adezmapimod (SB 203580) 是一种选择性的，ATP 竞争性的 p38 MAPK 抑制剂，对 SAPK2a/p38 和 SAPK2b/p38β2 的 IC50 分别为 50 nM 和 500 nM。Adezmapimod 抑制 LCK，GSK3β 和 PKBα，IC50 比 SAPK2a/p38 高 100-500 倍。Adezmapimod 不抑制 JNK 活性，是一种自噬 (autophagy) 和线粒体自噬 (mitophagy) 激活剂。

Adezmapimod(Synonyms: SB 203580; RWJ 64809)

Adezmapimod Chemical Structure

CAS No. : 152121-47-6

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 ￥600 In-stock
50 mg ￥1400 In-stock
100 mg ￥2400 In-stock
200 mg ￥3800 In-stock
500 mg   询价  
1 g   询价  

* Please select Quantity before adding items.

Adezmapimod 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus
  • Immunology/Inflammation Compound Library
  • Kinase Inhibitor Library
  • MAPK Compound Library
  • Anti-Cancer Compound Library
  • Autophagy Compound Library
  • Anti-Aging Compound Library
  • Reprogramming Compound Library
  • Oxygen Sensing Compound Library
  • Pyroptosis Compound Library
  • Anti-Lung Cancer Compound Library
  • Neurodegenerative Disease-related Compound Library
  • Angiogenesis Related Compound Library
  • Mitochondria-Targeted Compound Library

生物活性

Adezmapimod (SB 203580) is a selective and ATP-competitive p38 MAPK inhibitor with IC50s of 50 nM and 500 nM for SAPK2a/p38 and SAPK2b/p38β2, respectively. Adezmapimod inhibits LCK, GSK3β and PKBα with IC50s of 100-500-fold higher than that for SAPK2a/p38. Adezmapimod does not disrupt JNK activity and is an autophagy and mitophagy activator[1].

IC50 & Target[1]

p38

50 nM (IC50)

p38β2

500 nM (IC50)

体外研究
(In Vitro)

Adezmapimod (SB 203580) (preincubated with 0-30 μM for 1 h and cultured for 24 h in the presence of 20 ng/mL IL-2) prevents the IL-2-induced proliferation of primary human T cells, murine CT6 T cells, or BAF F7 B cells with an IC50 of 3-5 μM[1].
SB203580 blocks PKB phosphorylation (IC50 3-5 μM). SB203580 inhibitsthe phosphorylation of Ser473 in a dose-dependent manner in both CT6 and activated human T cells and IL-2-responsive BA/F3 F7 B cells[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 Proliferation Assay[1]

Cell Line: CT6, BA/F3 cell line F7, and PBMC/T cells
Concentration: 0-30 μM
Incubation Time: Preincubated with 0-30 μM SB203580 for 1 h and cultured for 24 h in the presence of 20 ng/mL IL-2
Result: Prevented the IL-2-induced proliferation of primary human T cells, murine CT6 T cells, or BAF F7 B cells with an IC50 of 3-5 μM.

Western Blot Analysis[1]

Cell Line: CT6 cells, activated human T cells, and BA/F3 F7 cells
Concentration: 0-30 μM
Incubation Time: Preincubated with 0-30 μM SB203580 for 1 h before stimulating with 20 ng/mL IL-2 for 5 min
Result: Inhibited the phosphorylation of PKB at Ser473 in a dose-dependent manner.

体内研究
(In Vivo)

Adezmapimod (SB 203580) (5 mg/kg/day; intra peritoneal injected daily for 16 consecutive days, in female atymic Nu/Nu mice) treatment, p38WT tumors show a significantly smaller tumor burden when compared with p38TM tumors that were treated in parallel[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 Model: Six-week-old female atymic Nu/Nu mice CAL27 p38WT and p38TM tumors[1]
Dosage: 5 mg/kg/day
Administration: Intra peritoneal injected daily for 16 consecutive days
Result: After 2 weeks treatment, CAL27 p38WT tumors were significantly smaller; CAL27 p38TM tumors were not affected by the p38 inhibitor (n=10).

分子量

377.43

Formula

C21H16FN3OS
CAS 号

152121-47-6
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 : 50 mg/mL (132.47 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.6495 mL 13.2475 mL 26.4950 mL
5 mM 0.5299 mL 2.6495 mL 5.2990 mL
10 mM 0.2649 mL 1.3247 mL 2.6495 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： 5% DMSO    40% PEG300    5% Tween-80    50% saline

    Solubility: ≥ 2.5 mg/mL (6.62 mM); Clear solution

  • 2.

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

    Solubility: ≥ 1.56 mg/mL (4.13 mM); Clear solution

    此方案可获得 ≥ 1.56 mg/mL (4.13 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 15.6 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: ≥ 1.56 mg/mL (4.13 mM); Clear solution

    此方案可获得 ≥ 1.56 mg/mL (4.13 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 15.6 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: ≥ 1.56 mg/mL (4.13 mM); Clear solution

    此方案可获得 ≥ 1.56 mg/mL (4.13 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 15.6 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]. Davies SP, et al. Specificity and mechanism of action of some commonly used protein kinase inhibitors. Biochem J. 2000 Oct 1;351(Pt 1):95-105.

    [2]. Lali FV, et al. The pyridinyl imidazole inhibitor SB203580 blocks phosphoinositide-dependent protein kinase activity, protein kinase B phosphorylation, and retinoblastoma hyperphosphorylation in interleukin-2-stimulated T cells independently of p38 mitogen-activated protein kinase. J Biol Chem. 2000 Mar 10;275(10):7395-402.

    [3]. Leelahavanichkul K, et al. A role for p38 MAPK in head and neck cancer cell growth and tumor-induced angiogenesis and lymphangiogenesis. Mol Oncol. 2014 Feb;8(1):105-18.

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

SB-431542

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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。

SB-431542  纯度: 99.89%

SB-431542 是一种有效，选择性的 ALK5/TGF-β type I Receptor 抑制剂，IC50 值为 94 nM。

SB-431542

SB-431542 Chemical Structure

CAS No. : 301836-41-9

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 ￥880 In-stock
10 mg ￥800 In-stock
50 mg ￥3380 In-stock
100 mg ￥6300 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

SB-431542 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus
  • Kinase Inhibitor Library
  • TGF-beta/Smad Compound Library
  • Anti-Cancer Compound Library
  • Reprogramming Compound Library
  • Anti-Pancreatic Cancer Compound Library
  • Angiogenesis Related Compound Library
  • Anti-Colorectal Cancer Compound Library

生物活性

SB-431542 is a potent and selective inhibitor of ALK5/TGF-β type I Receptor with an IC50 value of 94 nM[1].

IC50 & Target

ALK5

94 nM (IC50)

体外研究
(In Vitro)

SB-431542 (1 μM) significantly reduces the TGF-β-induced nuclear accumulation of Smad proteins in A498 cells. SB-431542 inhibits TGF-β1-induced collagen Iα1 and PAI-1 mRNA with IC50 values of 60 and 50 nM, respectively. In addition, SB-431542 inhibits TGF-β1-induced fibronectin mRNA and protein with IC50 values of 62 and 22 nM, respectively[1]. SB-431542 (10 μM) is a selective inhibitor of TGF-β signaling but has no effect on BMP signaling in NIH 3T3 cells[2]. TRKI, SB-431542, inhibits TGF-beta-induced transcription, gene expression, apoptosis, and growth suppression. SB-431542 attenuates the tumor-promoting effects of TGF-beta, including TGF-beta-induced EMT, cell motility, migration and invasion, and vascular endothelial growth factor secretion in human cancer cell lines. SB-431542 induces anchorage independent growth of cells that are growth-inhibited by TGF-beta, whereas it reduces colony formation by cells that are growth-promoted by TGF-beta[3]. SB-431542 (0.3 μM) inhibits cell proliferation induced by TGF-β in MG63 cells[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)

SB-431542 (10 mg/kg, i.p.) decreases lung metastasis but does not significantly alter growth of the primary tumor 4T1 xenograft[5].

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

384.39

Formula

C22H16N4O3
CAS 号

301836-41-9
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 : 250 mg/mL (650.38 mM; Need ultrasonic)

Ethanol : 11.17 mg/mL (29.06 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 2.6015 mL 13.0076 mL 26.0152 mL
5 mM 0.5203 mL 2.6015 mL 5.2030 mL
10 mM 0.2602 mL 1.3008 mL 2.6015 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 (5.41 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (5.41 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 (5.41 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (5.41 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
*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]. N. J. Laping, et al. Inhibition of Transforming Growth Factor (TGF)-β1-Induced Extracellular Matrix with a Novel Inhibitor of the TGF-β Type I Receptor Kinase Activity: SB-431542.

    [2]. Inman GJ, et al. SB-431542 is a potent and specific inhibitor of transforming growth factor-beta superfamily type I receptor-like kinase (ALK) receptors ALK4, ALK5, and ALK7. Mol Pharmacol, 2002, 62(1), 65-74.

    [3]. Halder SK, et al. A specific inhibitor of TGF-beta receptor kinase, SB-431542, as a potent antitumor agent for human cancers. Neoplasia, 2005, 7(5), 509-521.

    [4]. Matsuyama S, et al. SB-431542 inhibits transforming growth factor-beta-induced proliferation of human osteosarcoma cells. Cancer Res, 2003, 63(22), 7791-7798.

    [5]. Sato M, et al. Differential Proteome Analysis Identifies TGF-β-Related Pro-Metastatic Proteins in a 4T1 Murine Breast Cancer Model. PLoS One. 2015 May 18;10(5):e0126483.

    [6]. Ma J, et al. Growth differentiation factor 11 improves neurobehavioral recovery and stimulates angiogenesis in rats subjected to cerebral ischemia/reperfusion. Brain Res Bull. 2018 Feb 9;139:38-47
Kinase Assay
[3]

A total of 100,000 cells from each pool of A549 and HT29 are seeded into each well of 12-well plate. Cells are cultured in media containing 0.2% FBS for 18 hours, and then treated with 5 ng/mL TGF-β1 in the presence of SB-431542 (10 µM) in 0.5 mL of media for 24 hours. One hundred μLs of each supernatant media is used for VEGF assay according to the manufacturer’s instruction. For TGF-β1 ELISA, 100,000 cells from each pool of A549, VMRC-LCD, and HT29 are seeded into each well of 12-well plates and serum-starved for 20 hours. Cells are then treated with SB-431542 in 0.5 mL of serum-free RPMI media for 24 hours. One hundred μLs of each supernatant media is activated and used for TGF-β1 assay according to the manufacturer’s instruction.

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]

A498 cells are seeded at 5,000 to 10,000 cells/well in 96-well plates. The cells are serum-deprived for 24 h and then treated with SB-431542 for 48 h to assess the cellular toxicity. Cell viability is determined by incubating cells for 4 h with XTT labeling and electron coupling reagent according to the manufacturer’s directions. Live cells with active mitochondria produce an orange-colored product, formazan, which is detected using a plate reader at between A 450 nm and A 500 nm with a reference wavelength greater than 600 nm. The absorbance values correlate with the number of viable cells.

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
[5]

Ten thousand 4T1 cells are injected subcutaneously into the second mammary fat pad of 6-week-old Balb/c female mice. Tumors are measured twice weekly, and volume is calculated using the following formula: Volume = width2×length×0.52. Mice are randomly assigned to two treatment groups: control, n = 14 (20% DMSO/80% corn oil); SB-431542-treated, n = 15 (10 mg/kg body weight in 20% DMSO/80% corn oil, administered intraperitoneally three times per week starting one day after tumor cell inoculation. Primary tumors are resected when the volume at day 10 post-injection of 4T1 cells. All mice are monitored daily and euthanized after 4 weeks. The metastases are dissected to snap-freeze for further 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]. N. J. Laping, et al. Inhibition of Transforming Growth Factor (TGF)-β1-Induced Extracellular Matrix with a Novel Inhibitor of the TGF-β Type I Receptor Kinase Activity: SB-431542.

    [2]. Inman GJ, et al. SB-431542 is a potent and specific inhibitor of transforming growth factor-beta superfamily type I receptor-like kinase (ALK) receptors ALK4, ALK5, and ALK7. Mol Pharmacol, 2002, 62(1), 65-74.

    [3]. Halder SK, et al. A specific inhibitor of TGF-beta receptor kinase, SB-431542, as a potent antitumor agent for human cancers. Neoplasia, 2005, 7(5), 509-521.

    [4]. Matsuyama S, et al. SB-431542 inhibits transforming growth factor-beta-induced proliferation of human osteosarcoma cells. Cancer Res, 2003, 63(22), 7791-7798.

    [5]. Sato M, et al. Differential Proteome Analysis Identifies TGF-β-Related Pro-Metastatic Proteins in a 4T1 Murine Breast Cancer Model. PLoS One. 2015 May 18;10(5):e0126483.

    [6]. Ma J, et al. Growth differentiation factor 11 improves neurobehavioral recovery and stimulates angiogenesis in rats subjected to cerebral ischemia/reperfusion. Brain Res Bull. 2018 Feb 9;139:38-47

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

SB 202190

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。

SB 202190  纯度: 99.89%

SB 202190 是选择性的 p38 MAPK 抑制剂，抑制 p38α 和 p38β2 的 IC50 分别为 50 nM 和 100 nM。SB 202190 与重组人活性 p38 激酶的 ATP 袋结合，Kd 值为 38 nM。SB 202190 具有抗癌活性并可以挽救记忆障碍。

SB 202190

SB 202190 Chemical Structure

CAS No. : 152121-30-7

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 ￥627 In-stock
10 mg ￥570 In-stock
25 mg ￥995 In-stock
50 mg ￥1200 In-stock
100 mg ￥2000 In-stock
200 mg ￥3200 In-stock
500 mg   询价  
1 g   询价  

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SB 202190 相关产品

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  • Apoptosis Compound Library
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  • Kinase Inhibitor Library
  • MAPK Compound Library
  • Anti-Cancer Compound Library
  • Autophagy Compound Library
  • Reprogramming Compound Library
  • Oxygen Sensing Compound Library
  • Pyroptosis Compound Library
  • Anti-Lung Cancer Compound Library
  • Neurodegenerative Disease-related Compound Library
  • Angiogenesis Related Compound Library

生物活性

SB 202190 is a selective p38 MAP kinase inhibitor with IC50s of 50 nM and 100 nM for p38α and p38β2, respectively. SB 202190 binds to the ATP pocket of the active recombinant human p38 kinase with a Kd of 38 nM. SB 202190 has anti-cancer activity and rescued memory deficits[1][2]. SB202190 induces autophagy[3].

IC50 & Target[1]

p38α

50 nM (IC50)

p38β2

100 nM (IC50)

体外研究
(In Vitro)

SB 202190 (0-10 μM; 0-72 hours) attenuates growth of a subgroup of CRC cell lines such as RKO, CACO2 and SW480 in a dose- and time-dependent manner[1].
SB 202190 strongly inhibited colony formation and anchorage-independent growth (10 μM for 7–10 days) and elevated apoptotic cell death (10 μM for 72 h) in this same subset of CRC lines (RKO, CACO2 and SW480)[2].
In RKO, CACO2 and SW480 cells, SB202190 (10 μM; 2 hours) abrogates phosphorylation of S6K1(T389) and S6(S235/236), but not AKT(S473), indicating that p38i selectively blocks mTORC1 signaling[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)

SB 202190 (5 mg/kg; intraperitoneal injection; daily for 10-12 days) shows inhibition of tumor cell survival and tumor growth[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 Model: 4-week-old female BALB/c nude mice (bearing SW480 and RKO xenograft tumors)[2]
Dosage: 5 mg/kg
Administration: Intraperitoneal injection; daily for 10-12 days
Result: Inhibition of tumor cell survival and tumor growth.

分子量

331.34

Formula

C20H14FN3O
CAS 号

152121-30-7
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 : 100 mg/mL (301.80 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.0180 mL 15.0902 mL 30.1805 mL
5 mM 0.6036 mL 3.0180 mL 6.0361 mL
10 mM 0.3018 mL 1.5090 mL 3.0180 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 (6.28 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (6.28 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 (6.28 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (6.28 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 (6.28 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (6.28 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]. Davies SP, et al. Specificity and mechanism of action of some commonly used protein kinase inhibitors. Biochem J. 2000 Oct 1;351(Pt 1):95-105.

    [2]. Nemoto S, et al. Induction of apoptosis by SB202190 through inhibition of p38beta mitogen-activated protein kinase. J Biol Chem. 1998 Jun 26;273(26):16415-20.

    [3]. Grossi V, et al. Bay 43-9006 inhibits p38α activity in colorectal cancer cells and synergizes with the DFG-in inhibitor SB202190 to increase apoptotic response. Cancer Biol Ther. 2012 Dec;13(14):1471-81.

    [4]. Yang S, et al. Protective effects of p38 MAPK inhibitor SB202190 against hippocampal apoptosis and spatial learning and memory deficits in a rat model of vascular dementia. Biomed Res Int. 2013;2013:215798.

    [5]. Zhang Y, et al. PP2AC Level Determines Differential Programming of p38-TSC-mTOR Signaling and Therapeutic Response to p38-Targeted Therapy in Colorectal Cancer. EBioMedicine. 2015 Nov 19;2(12):1944-56.

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SBP-0636457(Synonyms: SBI-0636457; SB1-0636457)

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。

SBP-0636457 (Synonyms: SBI-0636457; SB1-0636457) 纯度: 98.42%

SBP-0636457 (SB1-0636457) 是一种 SMAC 模拟物，是 IAP 的拮抗剂。SBP-0636457 以 0.27 μM 的 Ki 与 IAP 蛋白的 BIR 结构域结合。SBP-0636457 可用于实体瘤和血液系统癌症的研究。

SBP-0636457(Synonyms: SBI-0636457; SB1-0636457)

SBP-0636457 Chemical Structure

CAS No. : 1422180-49-1

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5 mg ￥12000 In-stock
10 mg   询价  
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  • Bioactive Compound Library Plus

生物活性

SBP-0636457 (SB1-0636457) is a SMAC mimetic, and as an IAP antagonist. SBP-0636457 binds to the BIR-domains of the IAP proteins, with a Ki of 0.27 μM. SBP-0636457 can be used for the research of solid tumors and hematologic cancers[1][2].

IC50 & Target[1]

XIAP

0.27 μM (Ki)

体外研究
(In Vitro)

SBP-0636457 (1-20 μM) demonstrates no cytotoxicity in BT474, BT549, MCF7, and MDA-MB-231 breast cancer cell lines up to a concentration of 20μM[1].
SBP-0636457 (10-1000 nM; 20 h) is efficacious as TRAIL-sensitizing agents in MDA-MB-231 cells, with an EC50 of 9 nM[1].

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

456.58

Formula

C25H36N4O4
CAS 号

1422180-49-1
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

4°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
参考文献

  • [1]. Finlay D, et, al. Small-molecule IAP antagonists sensitize cancer cells to TRAIL-induced apoptosis: roles of XIAP and cIAPs. Mol Cancer Ther. 2014 Jan; 13(1): 5-15.

    [2]. Finlay D, et, al. Inducing death in tumor cells: roles of the inhibitor of apoptosis proteins. F1000Res. 2017 Apr 27; 6:587.

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SB225002

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。

SB225002  纯度: 99.87%

SB225002 是一种有效的选择性 CXCR2 非肽拮抗剂，抑制 125I-IL-8 和 CXCR2 结合的 IC50 为 22 nM。

SB225002

SB225002 Chemical Structure

CAS No. : 182498-32-4

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥605 In-stock
5 mg ￥550 In-stock
10 mg ￥770 In-stock
50 mg ￥2900 In-stock
100 mg ￥4900 In-stock
200 mg ￥7600 In-stock
500 mg   询价  
1 g   询价  

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SB225002 相关产品

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  • Covalent Screening Library
  • Endocrinology Compound Library

生物活性

SB225002, a potent, selective and non-peptide CXCR2 antagonist, inhibits 125I-IL-8 binding to CXCR2 with an IC50 of 22 nM.

IC50 & Target[1]

125I-IL-8-CXCR2

22 nM (IC50, in CHO cell membrane)

体外研究
(In Vitro)

SB225002 (SB 225002) is an antagonist of 125I-IL-8 binding to CXCR2 with an IC50=22 nM. SB225002 shows >150-fold selectivity over CXCR1 and four other 7-TMRs tested. SB225002 is a potent antagonist of rabbit CXCR2, inhibiting rabbit PMN chemotaxis in response to optimal concentrations of human IL-8 or GROα (IC50 values of 30 and 70 nM, respectively. In these cells (PMN, HL60, CXCR1-RBL-2H3), SB225002 produces a concentration-dependent inhibition of both IL-8- and GROα-mediated calcium mobilization with IC50 values of 8 and 10 nM, respectively. In 3ASubE cells stably transfected with CXCR2, SB 225002 dose-dependently inhibits calcium mobilization induced by both GROα and IL-8, with IC50 values of 20 and 40 nM, respectively[1]. WHCO1 cells treated with SB225002 exhibits a 40% reduction in cell proliferation. Blocking CXCR2 signaling in WHCO1 cells with 400 nM SB225002 (SB 225002) significantly decreases cell proliferation by ~40% to 50%[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)

SB225002 (SB 225002) selectively blocks IL-8-induced neutrophil margination in rabbits[1]. CXCR2 is blocked using the selective antagonist SB225002 (2 mg/kg) or neutralizing CXCR2 antiserum. The CXCR2 antagonist SB225002 decreases neutrophil counts in ischemic hemispheres of ApoE−/− mice on Western diet and wildtype mice on normal diet[3]. SB225002 significantly attenuates microglial activation and BBB damage, increases myelination, and reduces astrogliosis in the white matter after LPS-sensitized HI[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

352.14

Formula

C13H10BrN3O4
CAS 号

182498-32-4
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

4°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
溶解性数据
In Vitro: 

DMSO : ≥ 100 mg/mL (283.98 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 2.8398 mL 14.1989 mL 28.3978 mL
5 mM 0.5680 mL 2.8398 mL 5.6796 mL
10 mM 0.2840 mL 1.4199 mL 2.8398 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 (stored under nitrogen)。-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 (7.10 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (7.10 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 (7.10 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (7.10 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 (7.10 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (7.10 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]. White JR, et al. Identification of a potent, selective non-peptide CXCR2 antagonist that inhibits interleukin-8-induced neutrophil migration. J Biol Chem. 1998 Apr 24;273(17):10095-8.

    [2]. Wang B, et al. A growth-related oncogene/CXC chemokine receptor 2 autocrine loop contributes to cellular proliferation in esophageal cancer. Cancer Res. 2006 Mar 15;66(6):3071-7.

    [3]. Herz J, et al. Role of Neutrophils in Exacerbation of Brain Injury After Focal Cerebral Ischemia in Hyperlipidemic Mice. Stroke. 2015 Oct;46(10):2916-25.

    [4]. Wang LY, et al. CXCL5 signaling is a shared pathway of neuroinflammation and blood-brain barrier injury contributing to white matter injury in the immature brain. J Neuroinflammation. 2016 Jan 6;13:6.

    [5]. Shi ZR, et al. Decrease of galectin-3 in keratinocytes: A potential diagnostic marker and a critical contributor to the pathogenesis of psoriasis. J Autoimmun. 2018 May;89:30-40.
Kinase Assay
[1]

CHO-CXCR1 and CHO-CXCR2 membranes are prepared. Assays are performed in 96-well microtiter plates where the reaction mixture contained 1.0 μg/mL membrane protein in 20 mM Bis-Tris-propane, pH 8.0, with 1.2 mM MgSO4, 0.1 mM EDTA, 25 mM NaCl, and 0.03% CHAPS and SB 225002 (10 mM stock in Me2SO) added at the indicated concentrations, the final Me2SO concentration is <1% under standard binding conditions. Binding is initiated by addition of 0.25 nM 125I-IL-8 (2,200 Ci/mmol). After 1-h incubation at room temperature the plate is harvested using a Tomtec 96-well harvester onto a glass fiber filtermat blocked with 1% polyethyleneimine, 0.5% BSA and washed three times with 25 mM NaCl, 10 mM Tris•HCl, 1 mM MgSO4, 0.5 mMEDTA, 0.03% CHAPS, pH 7.4. The filter is dried, sealed in a sample bag containing 10 mL of Wallac 205 Betaplate liquid scintillation fluid, and counted with a Wallac 1205 Betaplate liquid scintillation counter[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
[2]

Three esophageal squamous cell carcinoma cell lines WHCO1, WHCO5, and WHCO6 originally established from surgical biopsies of primary esophageal squamous cell carcinomas are cultured in DMEM containing 10% FCS at 37°C in a humidified atmosphere of 5% CO2. MTT assays are carried out using the Cell Proliferation kit. Briefly, 1.5×103 cells are plated in 96-well plates in a final volume of 180 μL DMEM per well. SB 225002 (400 nM) is added to cells and 0.001% DMSO (solvent) is added as a control. After the indicated incubation period, 18 μL of the MTT labeling reagent (final concentration 0.5 mg/mL) is added to each well and incubated for 4 hours in a humidified atmosphere. One hundred eighty microliters of the solubilization solution are added to each well and the plates are left overnight at 37°C. The spectrophotometric absorbance of samples is measured at 595 nm using a microtiter plate 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][4]

Mice[3]
Male 7-8 weeks old wildtype (C57BL/6J, Harlan) and ApoE−/− mice, which are generated on the same C57BL/6 background, are either fed with a normal chow or a cholesterol rich chow for 6 weeks and submitted to 20 min of left-sided middle cerebral artery occlusion (MCAO) or sham surgery. Animals are randomly attributed to treatment paradigms, and experimenters are blinded at all stages of interventions and data analysis. The selective CXCR2 antagonist SB225002 (2 mg/kg) or vehicle (1% DMSO in PBS) is injected intraperitoneally (i.p.) at 0, 24 and 48 hours post-ischemia. In other experiments, CXCR2 is specifically blocked by i.p. injection of a neutralizing rabbit anti-CXCR2 serum (300 μL) at 0 hours, 24 hours and 48 hours post-ischemia. In the latter studies, normal rabbit serum (NRS) served as control. In some experiments, neutrophils are depleted by i.p. injection of 200 μg anti-mouse Ly6G 24 hours before and 24 hours after ischemia. In these experiments, 200 μg of an isotype control antibody is delivered as control.
Rats[4]
In this study, 10-12 Sprague-Dawley rat pups per dam are used. The pups receive intraperitoneal injections of SB225002 (1 or 3 mg/kg, diluted in NS containing 0.33 % Tween 80) or vehicle (NS solution containing 0.33 % Tween 80) 30 min before lipopolysaccharide (LPS) administration and immediately after hypoxic ischemia (HI). The pups are randomly assigned to four groups: control (pups unexposed to LPS or HI, N=14), vehicle (NS injections 30 min before LPS administration and immediately after HI, N=18), and SB-1 (1 mg/kg, N=14) and SB-3 (3 mg/kg, N=18) (SB225002 injections 30 min before LPS administration and immediately after HI).

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]. White JR, et al. Identification of a potent, selective non-peptide CXCR2 antagonist that inhibits interleukin-8-induced neutrophil migration. J Biol Chem. 1998 Apr 24;273(17):10095-8.

    [2]. Wang B, et al. A growth-related oncogene/CXC chemokine receptor 2 autocrine loop contributes to cellular proliferation in esophageal cancer. Cancer Res. 2006 Mar 15;66(6):3071-7.

    [3]. Herz J, et al. Role of Neutrophils in Exacerbation of Brain Injury After Focal Cerebral Ischemia in Hyperlipidemic Mice. Stroke. 2015 Oct;46(10):2916-25.

    [4]. Wang LY, et al. CXCL5 signaling is a shared pathway of neuroinflammation and blood-brain barrier injury contributing to white matter injury in the immature brain. J Neuroinflammation. 2016 Jan 6;13:6.

    [5]. Shi ZR, et al. Decrease of galectin-3 in keratinocytes: A potential diagnostic marker and a critical contributor to the pathogenesis of psoriasis. J Autoimmun. 2018 May;89:30-40.

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

SB 216763

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。

SB 216763  纯度: 99.30%

SB 216763是有效，选择性和ATP竞争性的 GSK-3 抑制剂，抑制GSK-3α和GSK-3β的 IC50 为34.3 nM。

SB 216763

SB 216763 Chemical Structure

CAS No. : 280744-09-4

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 ￥715 In-stock
5 mg ￥650 In-stock
10 mg ￥1100 In-stock
50 mg ￥4800 In-stock
100 mg ￥7886 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

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  • Anti-Alzheimer’s Disease Compound Library
  • Anti-Pancreatic Cancer Compound Library
  • Anti-Cancer Metabolism Compound Library
  • Neurodegenerative Disease-related Compound Library
  • Glucose Metabolism Compound Library

生物活性

SB 216763 is potent, selective and ATP-competitive GSK-3 inhibitor with IC50s of 34.3 nM for both GSK-3α and GSK-3β.

IC50 & Target[5]

GSK-3α

34.3 nM (IC50)

GSK-3β

34.3 nM (IC50)

体外研究
(In Vitro)

SB-216763 (10-20 µM) induces β-catenin mediated-transcription in a dose-dependent manner in HEK293 cells. SB-216763 (10, 15 and 20 µM) can maintain mESCs with a pluripotent-like morphology in long-term culture. SB-216763 (10 µM) can maintain J1 mESCs in a pluripotent state for more than a month[2]. SB-216763 inhibits GSK-3 with IC50 of 34 nM[3]. SB-216763 is equally effective at inhibiting human GSK-3α and GSK-3β[5].

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)

SB216763 (20 mg/kg, i.v.) significantly improves the survival of BLM-treated mice. Mice randomized to receive BLM plus SB216763 shows a noteworthy reduction, compared with BLM-treated mice. SB216763 (20 mg/kg, i.v.) reduces the magnitude of BLM-induced alveolitis[1]. SB 216763 (0.2 mg/kg, i.v.) with either 17β-E100 or Geni100 reverses the ceiling effect because these agents significantly reduce infarct size when the rabbits’ hearts are submitted to 30-min CAO[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

371.22

Formula

C19H12Cl2N2O2
CAS 号

280744-09-4
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 : 100 mg/mL (269.38 mM; Need ultrasonic)

H2O : < 0.1 mg/mL (insoluble)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.6938 mL 13.4691 mL 26.9382 mL
5 mM 0.5388 mL 2.6938 mL 5.3876 mL
10 mM 0.2694 mL 1.3469 mL 2.6938 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 (6.73 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (6.73 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 (6.73 mM); Suspended solution; Need ultrasonic

    此方案可获得 2.5 mg/mL (6.73 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 (6.73 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (6.73 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]. Gurrieri, et al. 3-(2,4-dichlorophenyl)-4-(1-methyl-1H-indol-3-yl)-1H-pyrrole-2,5-dione (SB216763), a glycogen synthase kinase-3 inhibitor, displays therapeutic properties in a mouse model of pulmonary inflammation and fibrosis. J.Pharmacol.Exp.Ther.2010

    [2]. Kirby LA, et al. Glycogen synthase kinase 3 (GSK3) inhibitor, SB-216763, promotes pluripotency in mouse embryonic stem cells.PLoS One. 2012;7(6):e39329. Epub 2012 Jun 26.

    [3]. Wang M, et al. The first synthesis of [(11)C]SB-216763, a new potential PET agent for imaging of glycogen synthase kinase-3 (GSK-3).Bioorg Med Chem Lett. 2011 Jan 1;21(1):245-9. Epub 2010 Nov 11.

    [4]. The ceiling effect of pharmacological postconditioning with the phytoestrogen genistein is reversed by the GSK3beta inhibitor SB 216763 [3-(2,4-dichlorophenyl)-4(1-methyl-1H-indol-3-yl)-1H-pyrrole-2,5-dione] through mitochondrial ATP-dependent potassium channel opening.

    [5]. Coghlan MP, et al. Selective small molecule inhibitors of glycogen synthase kinase-3 modulate glycogen metabolism and gene transcription. Chem Biol. 2000 Oct;7(10):793-803.

    [6]. Wang W, et al. Inhibition of glycogen synthase kinase 3beta ameliorates triptolide-induced acute cardiac injury by desensitizing mitochondrial permeability transition. Toxicol Appl Pharmacol. 2016 Dec 15;313:195-203.
Cell Assay
[2]

MESCs maintained with LIF or 10 µM SB-216763 for more than a month are resuspended at 40,000 cells/mL in LIF-free mESC medium. EBs are prepared by a hanging drop procedure. Briefly, 20 µL drops containing mESCs are pipetted on the inside of a 10-cm Petri dish lid. The lids are placed onto Petri dishes containing 10 mL of HBSS and the EBs are allowed to form and grow for 4 days in the incubator. After 4 days, 15-20 EBs are transferred to a well containing LIF-free mESC medium in a 24-well plate. The medium is exchanged every two days and autonomously beating cell aggregates are observed and counted.

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]

Mice are allocated to four groups (n=12/group) as follows: 1) intratracheal saline + vehicle (25% dimethyl sulfoxide, 25% polyethylene glycol, and 50% saline), 2) intratracheal saline + SB216763 (20 mg/kg) dissolved in vehicle, 3) intratracheal BLM (3 U/kg) + vehicle, and 4) intratracheal BLM + SB216763 (20 mg/kg) in vehicle. Another set of experiments to assess cytokine expression by reverse transcription-PCR is conducted in the mice (n=12/group) to receive 1) intratracheal saline + vehicle, 2) intratracheal BLM, and 3) intratracheal BLM + SB216763. To induce pulmonary fibrosis, BLM is intratracheally administered in mice (n=15/group) on day 0. BLM and saline-treated mice are administered with SB216763 dissolved in vehicle or vehicle alone intravenously at day 0 and then intraperitoneally twice a week until day 28. Mice are sacrificed by CO2 inhalation on days 2, 7, and 28. In the terminal deoxynucleotidyl transferase dUTP nick-end labeling (TUNEL) experiments, the cohorts of mice are as follows: saline-treated (n=6), BLM-treated (n=6), and BLM + SB216763-treated (n=6).

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]. Gurrieri, et al. 3-(2,4-dichlorophenyl)-4-(1-methyl-1H-indol-3-yl)-1H-pyrrole-2,5-dione (SB216763), a glycogen synthase kinase-3 inhibitor, displays therapeutic properties in a mouse model of pulmonary inflammation and fibrosis. J.Pharmacol.Exp.Ther.2010

    [2]. Kirby LA, et al. Glycogen synthase kinase 3 (GSK3) inhibitor, SB-216763, promotes pluripotency in mouse embryonic stem cells.PLoS One. 2012;7(6):e39329. Epub 2012 Jun 26.

    [3]. Wang M, et al. The first synthesis of [(11)C]SB-216763, a new potential PET agent for imaging of glycogen synthase kinase-3 (GSK-3).Bioorg Med Chem Lett. 2011 Jan 1;21(1):245-9. Epub 2010 Nov 11.

    [4]. The ceiling effect of pharmacological postconditioning with the phytoestrogen genistein is reversed by the GSK3beta inhibitor SB 216763 [3-(2,4-dichlorophenyl)-4(1-methyl-1H-indol-3-yl)-1H-pyrrole-2,5-dione] through mitochondrial ATP-dependent potassium channel opening.

    [5]. Coghlan MP, et al. Selective small molecule inhibitors of glycogen synthase kinase-3 modulate glycogen metabolism and gene transcription. Chem Biol. 2000 Oct;7(10):793-803.

    [6]. Wang W, et al. Inhibition of glycogen synthase kinase 3beta ameliorates triptolide-induced acute cardiac injury by desensitizing mitochondrial permeability transition. Toxicol Appl Pharmacol. 2016 Dec 15;313:195-203.

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

SB-633825

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。

SB-633825  纯度: 98.17%

SB-633825 是有效的， ATP 竞争性的 TIE2，LOK (STK10) 和 BRK 抑制剂，IC50 分别为 3.5 nM，66 nM 和 150 nM。SB-633825 抑制癌细胞的生长和血管生成。

SB-633825

SB-633825 Chemical Structure

CAS No. : 956613-01-7

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥4260 In-stock
5 mg ￥4000 In-stock
10 mg ￥6800 In-stock
50 mg ￥19000 In-stock
100 mg ￥30000 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

SB-633825 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus
  • Anti-Cancer Compound Library
  • Anti-Cardiovascular Disease Compound Library

生物活性

SB-633825 is a potent and ATP-competitive inhibitor of TIE2, LOK (STK10) and BRK with IC50s of 3.5 nM, 66 nM, 150 nM, respectively. SB-633825 can inhibit cancer cell growth and angiogenesis[1].

IC50 & Target

IC50: 3.5 nM (TIE2), 66 nM (LOK) and 150 nM (BRK)[1]
体外研究
(In Vitro)

SB-633825 inhibits TIE2 Tyrosine-protein kinase (TIE2), lymphocyte-oriented kinase (LOK; STK10) and breast tumor kinase (Brk; PTK6)[1].
SB-633825 inhibits LOK to 44% maximal activity and TIE2 to 75% maximal activity at 0.1 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.
分子量

483.58

Formula

C28H25N3O3S
CAS 号

956613-01-7
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 : 9.62 mg/mL (19.89 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.0679 mL 10.3396 mL 20.6791 mL
5 mM 0.4136 mL 2.0679 mL 4.1358 mL
10 mM 0.2068 mL 1.0340 mL 2.0679 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]. Elkins JM, et al. Comprehensive characterization of the Published Kinase Inhibitor Set. Nat Biotechnol. 2016 Jan;34(1):95-103.

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

SB 525334

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。

SB 525334  纯度: 99.96%

SB 525334是一种有效，选择性的转化生长因子β1受体 (ALK5) 抑制剂，IC50 为 14.3 nM。

SB 525334

SB 525334 Chemical Structure

CAS No. : 356559-20-1

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 ￥616 In-stock
5 mg ￥560 In-stock
10 mg ￥880 In-stock
50 mg ￥3348 In-stock
100 mg ￥6000 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

SB 525334 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus
  • Kinase Inhibitor Library
  • TGF-beta/Smad Compound Library
  • Anti-Cancer Compound Library
  • Reprogramming Compound Library
  • Anti-Pancreatic Cancer Compound Library
  • Angiogenesis Related Compound Library
  • Anti-Colorectal Cancer Compound Library

生物活性

SB 525334 is a potent and selective transforming growth factor β1 receptor (ALK5) inhibitor with an IC50 of 14.3 nM.

IC50 & Target

IC50: 14.3 nM (ALK5)[1]
体外研究
(In Vitro)

SB525334 (1 μM; for 15 minutes before stimulating with 0.625 ng/ml of TGF-β1, assesses after 6 days) inhibits TGF-β1-mediated proliferation of familial idiopathic pulmonary arterial hypertension (iPAH) pulmonary artery smooth muscle cells (PASMCs) at an IC50 of 295 nM [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.

Cell Proliferation Assay[2]

Cell Line: PASMC cells
Concentration: 1 μM
Incubation Time: Pre-incubated for 15 minutes (before stimulating with 0.625 ng/ml of TGF-β1), assessed after 6 days
Result: Inhibited TGF-β1-mediated proliferation of familial iPAH PASMCs at an IC50 of 295 nM.

体内研究
(In Vivo)

SB525334 (3-30 mg/kg; p.o.; daily from days 17 to 35) significantly reverses pulmonary arterial pressure in a rat model of pulmonary arterial hypertension (PAH)[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 Model: Adult male Sprague-Dawley rats (MCT rat model of pulmonary hypertension)[2]
Dosage: 3, 30 mg/kg
Administration: Oral administration; daily from days 17 to 35
Result: Reduced the proportion of fully muscularized vessels to 28% at 3 mg/kg and returned fully muscularized vessel distribution beyond that seen at day 17 and approaching the phenotype observed in saline-exposed controls at 30 mg/kg.

分子量

343.42

Formula

C21H21N5
CAS 号

356559-20-1
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 (291.19 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.9119 mL 14.5594 mL 29.1189 mL
5 mM 0.5824 mL 2.9119 mL 5.8238 mL
10 mM 0.2912 mL 1.4559 mL 2.9119 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 (7.28 mM); Clear solution

    此方案可获得 ≥ 2.5 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 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 (7.28 mM); Clear solution

    此方案可获得 ≥ 2.5 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 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
*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]. Grygielko ET, et al. Inhibition of gene markers of fibrosis with a novel inhibitor of transforming growth factor-beta type I receptor kinase in puromycin-induced nephritis. J Pharmacol Exp Ther, 2005, 313(3), 943-951.

    [2]. Thomas M, et al. ALK5 mediates abnormal proliferation of vascular smooth muscle cells from patients with familial pulmonary arterial hypertension and is involved in the progression of experimental pulmonary arterial hypertension induced by monocrotaline. Am J Pathol, 2009, 174(2), 380-389.

    [3]. Laping NJ, et al. Tumor-specific efficacy of transforming growth factor-beta RI inhibition in Eker rats. Clin Cancer Res, 2007, 13(10), 3087-3899.

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

SB300实验室大容量电加热板

发表于由

【简单介绍】

品牌 金畔 加工定制 否

英国Stuart SB300实验室大容量电加热板（硅铝合金面板）采用铝硅合金材料的台面，具有良好的防撞性和耐磨性，以及极好的热传导性，加热迅速，保证整个台面温度均匀*。

进口，！

【详细说明】

SB300实验室大容量电加热板

产品描述

    英国Stuart实验室大容量电加热板SB300（硅铝合金面板）采用铝硅合金材料的台面，具有良好的防撞性和耐磨性，以及极好的热传导性，加热迅速，保证整个台面温度均匀*。

产品特点：

良好化学稳定性的玻璃陶瓷表面；或硬质铝硅合金台面，坚固耐用
大台面，用于加热大烧瓶或数个小烧瓶，z大处理10升的烧杯或烧瓶
的安全设计，包括：温度提示灯闪烁和溢出保护控制设计
微处理器控制温度准确，快速加热，z高温度达300℃或450℃
表面温度超过50℃时提示灯闪烁

技术参数：

产品编号 SB300
控制方式 模拟控制
加热板材料 铝硅合金
加热板规格 300×300mm
加热面积 300×300mm
加热功率 600W
外形规格（宽×D×H） 300×360×105mm
使用温度高达 300℃
乘重能力 6kg
电源 230V/50-60Hz,600W

SB300实验室大容量电加热板

 

相关产品：

SD160数字式加热板16×16cm

Undergrad系列加热板UC150和US150

聚四氟乙烯加热板CP300

红外加热板CR300

 

 

 

加热板附件（如下：）

型号：

防护盖：
经济的防止化学品爆沸的装置 
对大多数的化学品和溶剂具有相当良好的耐受性 
由Esco?硅胶生成

油浴/水浴：
结实的铝合金结构，是采用玻璃容器安全的选择 
酚醛树脂材料制造的提手把柄 
在加热板上四角支撑，安全可靠 
达到2升的容量

沙浴：
结实的铝合金构造 
特别适合于干燥加热的试管或者其它容器 
在加热板上四角支撑，安全可靠 
达到1升的容量

圆底烧瓶铝块：
转换加热器成为电热帽 
结实的铝合金构造，四角支撑，安全可靠 
适合于四个不同的规格圆底烧瓶，25ml，50ml，100ml和250ml 
可使用预先设置的孔安装温度计或采用其它类型的温度探头 

订货编号：

产品型号 产品描述
SB16/1 防护盖，用于加热器/搅拌器
SB16/2 防护盖，用于模拟控制的加热器/搅拌器
SB16/3 防护盖，用于数字控制的加热器/搅拌器
SB16/4 防护盖，用于数字控制的加热器
SB16/5 油浴/水浴
SB16/6 圆底烧瓶铝块
SB16/7 沙浴
SR1 曲颈瓶，600×12mm直径
 

 

英国Stuart-大容量模拟控制电加热器CB300/SB300

发表于由

【简单介绍】

品牌 金畔 加工定制 否

英国Stuart大容量模拟控制电加热器CB300/SB300：
CB30型采用玻璃陶瓷材料作为台面，具有优良的化学耐受性和更高的加热温度，平滑的表面容易清理，不生锈或腐蚀，因此无污染物停留，现代风格的白色表面使样品的颜色改变的观察变得容易、清晰。

SB300型采用铝硅合金材料的台面，具有良好的防撞性和耐磨性，以及极好的热传导性，加热迅速，保证整个台面温度均匀*。

【详细说明】

英国Stuart大容量模拟控制电加热器CB300/SB300

产品分别描述：

  CB300型采用玻璃陶瓷材料作为台面，具有优良的化学耐受性和更高的加热温度，平滑的表面容易清理，不生锈或腐蚀，因此无污染物停留，现代风格的白色表面使样品的颜色改变的观察变得容易、清晰。

  SB300型采用铝硅合金材料的台面，具有良好的防撞性和耐磨性，以及极好的热传导性，加热迅速，保证整个台面温度均匀性。

英国Stuart大容量模拟控制电加热器CB300/SB300

产品特点：

  1. 大台面，用于加热大烧瓶或数个小烧瓶，z大处理10升的烧杯或烧瓶
  2. 良好化学稳定性的玻璃陶瓷表面；或硬质铝硅合金台面，坚固耐用
  3. 的安全设计，包括：温度提示灯闪烁和溢出保护控制设计
  4. 表面温度超过50℃时提示灯闪烁
  5. 微处理器控制温度准确，快速加热，z高温度达300℃或450℃

技术参数：

产品编号 CB300 SB300
控制方式 模拟控制 模拟控制
加热板材料 玻璃陶瓷 铝硅合金
加热板规格 300×300mm 300×300mm
加热面积 200×200mm 300×300mm
加热功率 1200W 600W
外形规格（宽×D×H） 300×360×105mm 300×360×105mm
z高使用温度 450℃ 300℃
乘重能力 6kg 6kg
电源 230V/50-60Hz,1200W 230V/50-60Hz,600W

 

 

相关产品：

SD160数字式加热板16×16cm

Undergrad系列加热板UC150和US150

聚四氟乙烯加热板CP300

红外加热板CR300

 

 

 

加热板附件（如下：）

型号：

防护盖：
经济的防止化学品爆沸的装置 
对大多数的化学品和溶剂具有相当良好的耐受性 
由Esco?硅胶生成

油浴/水浴：
结实的铝合金结构，是采用玻璃容器安全的选择 
酚醛树脂材料制造的提手把柄 
在加热板上四角支撑，安全可靠 
达到2升的容量

沙浴：
结实的铝合金构造 
特别适合于干燥加热的试管或者其它容器 
在加热板上四角支撑，安全可靠 
达到1升的容量

圆底烧瓶铝块：
转换加热器成为电热帽 
结实的铝合金构造，四角支撑，安全可靠 
适合于四个不同的规格圆底烧瓶，25ml，50ml，100ml和250ml 
可使用预先设置的孔安装温度计或采用其它类型的温度探头 

订货编号：

产品型号 产品描述
SB16/1 防护盖，用于加热器/搅拌器
SB16/2 防护盖，用于模拟控制的加热器/搅拌器
SB16/3 防护盖，用于数字控制的加热器/搅拌器
SB16/4 防护盖，用于数字控制的加热器
SB16/5 油浴/水浴
SB16/6 圆底烧瓶铝块
SB16/7 沙浴
SR1 曲颈瓶，600×12mm直径
 

 

英国Stuart-超大容量加热板CB500/SB500（模拟控制）

发表于由

【简单介绍】

品牌 金畔 加工定制 否

英国Stuart超大容量加热板CB500/SB500（模拟控制）：CB500型采用玻璃陶瓷材料作为台面，易清理；由于*的热性能, 它可以在很短的时间内加热到很高的温度。
SB500型采用铝硅合金材料的台面，具有极好的热传导性，加热迅速，保证整个台面温度均匀*。

进口，！

【详细说明】

英国Stuart超大容量加热板CB500/SB500（模拟控制）

产品概述：

   这种长方形的加热器非常适合于同时加热多个小容器。例如，在教学中，需要同时加热学生们的样品。

位于加热器前面的旋钮用来控制加热板的温度，非常容易使用。

加热区域在使用后，热度仍会保持一段时间。为了安全起见，红色“HOT”高温提示灯会一直闪烁知道加热板冷却下来。

产品分别描述：
CB500型采用玻璃陶瓷材料作为台面，易清理；由于*的热性能, 它可以在很短的时间内加热到很高的温度。
SB500型采用铝硅合金材料的台面，具有极好的热传导性，加热迅速，保证整个台面温度均匀*。

产品特点：

  1. z多可同时处理30个100ml的烧瓶
  2. 可供选择的加热板材料：玻璃陶瓷加热板,或硬质铝硅合金加热板
  3. 大台面，用于加热数个烧瓶
  4. 微处理器控制温度准确，快速加热准确，z高温度达300℃或450℃
    英国Stuart超大容量加热板CB500/SB500（模拟控制）

技术参数

产品编号 CB500 SB500
控制方式 模拟控制 模拟控制
加热板材料 玻璃陶瓷 铝硅合金
加热板规格 300×500mm 300×500mm
加热面积 250×450mm 300×500mm
加热功率 2250W 1500W
外形规格（宽×D×H） 520×360×130 520×360×130
z高使用温度 375℃ 300℃
净重 12kg 12kg
电源 230V/50Hz,2250W 230V/50Hz,1500W
 
IP等级 31 31

订货信息

产品型号 产品描述
CB500 加热板，玻璃陶瓷台面，模拟式
SB500 加热板，玻璃陶瓷台面，模拟式
SR3 支撑杆托
SR1 支撑杆，600×12mm（直径）

 

相关产品：

SD160数字式加热板16×16cm

Undergrad系列加热板UC150和US150

聚四氟乙烯加热板CP300

红外加热板CR300

 

 

 

加热板附件（如下：）

型号：

防护盖：
经济的防止化学品爆沸的装置 
对大多数的化学品和溶剂具有相当良好的耐受性 
由Esco?硅胶生成

油浴/水浴：
结实的铝合金结构，是采用玻璃容器安全的选择 
酚醛树脂材料制造的提手把柄 
在加热板上四角支撑，安全可靠 
达到2升的容量

沙浴：
结实的铝合金构造 
特别适合于干燥加热的试管或者其它容器 
在加热板上四角支撑，安全可靠 
达到1升的容量

圆底烧瓶铝块：
转换加热器成为电热帽 
结实的铝合金构造，四角支撑，安全可靠 
适合于四个不同的规格圆底烧瓶，25ml，50ml，100ml和250ml 
可使用预先设置的孔安装温度计或采用其它类型的温度探头 

订货编号：

产品型号 产品描述
SB16/1 防护盖，用于加热器/搅拌器
SB16/2 防护盖，用于模拟控制的加热器/搅拌器
SB16/3 防护盖，用于数字控制的加热器/搅拌器
SB16/4 防护盖，用于数字控制的加热器
SB16/5 油浴/水浴
SB16/6 圆底烧瓶铝块
SB16/7 沙浴
SR1 曲颈瓶，600×12mm直径
 

 

Relacatib(Synonyms: SB-462795)

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。

Relacatib (Synonyms: SB-462795)

Relacatib (SB-462795) 是一种新的，有效的口服活性的人组织蛋白酶 K, L 和 V (cathepsins K, L, V) 的抑制剂，其Ki 值分别为 41, 68 和 53 pM。Relacatib 原位抑制人破骨细胞内源性组织蛋白酶 K 和人破骨细胞介导的骨吸收，IC50 值分别为 45 nM 和 70 nM。Relacatib 对体外人体组织骨吸收的抑制作用，以及对食蟹猴体内骨吸收有抑制作用。

Relacatib(Synonyms: SB-462795)

Relacatib Chemical Structure

CAS No. : 362505-84-8

规格 价格 是否有货
5 mg ￥11500 询问价格 & 货期

* Please select Quantity before adding items.

生物活性

Relacatib (SB-462795) is a novel, potent, and orally active inhibitor of human cathepsins K, L, and V with Ki values of 41 pM, 68 pM, and 53 pM, respectively. Relacatib inhibits endogenous cathepsin K in situ in human osteoclasts and human osteoclast-mediated bone resorption with IC50 values of 45 nM and 70 nM, respectively. Relacatib inhibits bone resorption in vitro in human tissue as well as in cynomolgus monkeys in vivo[1][2].

IC50 & Target

Ki: 41 pM (cathepsins K)
68 pM (cathepsins L)
53 pM (cathepsins V)[1]
体外研究
(In Vitro)

Relacatib are incubated with human osteoclastoma-derived osteoclasts seeded onto bovine cortical bone slices in vitro biological activity, it shows inhibitory potency with Ki values of 0.041 nM, 0.068 nM,0.063 nM,1.6 nM,and 13 nM against human cathepsin K, cathepsin L, cathepsin V, cathepsin S and cathepsin B, respectively in the assay[1].
Relacatib is against Monkey cathepsin K, cathepsin L,cathepsin V and cathepsin B with Ki values of 0.041 nM, 0.28 nM, 0.72 nM and 11nM, respectively. Relacatib is against mouse cathepsin L and rat cathepsin L with Ki values of 0.20 nM and 0.17 nM, respectively[2].

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)

Relacatib (1-2 mg/kg 0.5 h intravenous infusion; 2-4 mg/kg oral bolus gavage) exhibits T1/2, CL or Vdss with 109 mins, 19.5 mL/min/kg, or 1.86 L/kg in male Sprague-Dawley rats and 168 mins, 11.7 mL/min/kg, and 1.79 L/kg in monkeys, respectively in a PK iv/po crossover studies. The oral bioavailability of Relacatib is 28% in the monkey and 89.4% in the rats[1].
SB-462795 (subcutaneous injection; 12 mg/kg; blood sample is drawn 1.5, 4, 24, 48, and 72 h post dose administration) significantly inhibits resorption as assessed by two markers of bone resorption,the N- (NTx) and C-telopeptides (CTx) of type I collagen measured in serum. SB-462795 does not exhibit difference of serum osteocalcin (a biomarker of osteoblast activity) between SB-462795 and vehicle treated animalsexcept for the 48 h time point where a significant reduction (42% lower than baseline vs. 18% lower than baseline with vehicle treatment)[2].

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

Animal Model: Cynomolgus monkey[2]
Dosage: 12 mg/kg
Administration: Subcutaneous injection; single dose; blood sample is drawn 1.5, 4, 24, 48, and 72 h post dose administration
Result: Was sufficiently high to significantly suppress bone resorption from 1.5 to 72 h post dosing.

Clinical Trial

分子量

540.63

Formula

C27H32N4O6S
CAS 号

362505-84-8
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.
溶解性数据
In Vivo:
  • 1.

    SSB-462795 is prepared as a nanosuspension containing 1.5% Methylcellulose and 2.0% sodium lauryl sulfate[2].

  • 2.

    SB-462795 (12 mg/kg) or vehicle is in 70% aqueous PEG400(1 ml/kg)[2].
参考文献

  • [1]. Dennis S Yamashita, et al. Structure Activity Relationships of 5-, 6-, and 7-methyl-substituted azepan-3-one Cathepsin K Inhibitors.J Med Chem

    [2]. S Kumar, et al.A Highly Potent Inhibitor of Cathepsin K (Relacatib) Reduces Biomarkers of Bone Resorption Both in Vitro and in an Acute Model of Elevated Bone Turnover in Vivo in Monkeys.Bone. 2007 Jan;40(1):122-31.

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

SB1-G-187

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。

SB1-G-187 

SB1-G-187 是一种 PROTAC，一种多激酶降解剂。

SB1-G-187

SB1-G-187 Chemical Structure

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

SB1-G-187, a PROTAC, is a multi-kinase degrader[1].

分子量

1022.03

Formula

C52H54F3N9O10
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

-20°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
溶解性数据
In Vitro: 

DMSO : 100 mg/mL (97.84 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 0.9784 mL 4.8922 mL 9.7844 mL
5 mM 0.1957 mL 0.9784 mL 1.9569 mL
10 mM 0.0978 mL 0.4892 mL 0.9784 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 (stored under nitrogen)。-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: 5 mg/mL (4.89 mM); Suspended solution; Need ultrasonic

    此方案可获得 5 mg/mL (4.89 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 50.0 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: ≥ 5 mg/mL (4.89 mM); Clear solution

    此方案可获得 ≥ 5 mg/mL (4.89 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 50.0 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 Shanghai Jinpan Biotech Co Ltd 网站选购。
参考文献

  • [1]. Katherine A Donovan, et al. Mapping the Degradable Kinome Provides a Resource for Expedited Degrader Development. Cell. 2020 Dec 10;183(6):1714-1731.e10.

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

SB-743921 hydrochloride

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。

SB-743921 hydrochloride  纯度: 98.11%

SB-743921 hydrochloride 是一种有效的驱动蛋白 (Eg5) 抑制剂，Ki 值为 0.1 nM。

SB-743921 hydrochloride

SB-743921 hydrochloride Chemical Structure

CAS No. : 940929-33-9

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥1461 In-stock
5 mg ￥1200 In-stock
10 mg ￥2050 In-stock
50 mg ￥6450 In-stock
100 mg ￥9500 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

SB-743921 hydrochloride 相关产品

•相关化合物库:

  • Drug Repurposing Compound Library Plus
  • Clinical Compound Library Plus
  • Bioactive Compound Library Plus
  • Cell Cycle/DNA Damage Compound Library
  • Anti-Cancer Compound Library
  • Clinical Compound Library
  • Anti-Aging Compound Library
  • Drug Repurposing Compound Library
  • Anti-COVID-19 Compound Library
  • Cytoskeleton Compound Library
  • Anti-Lung Cancer Compound Library
  • Anti-Blood Cancer Compound Library

生物活性

SB-743921 hydrochloride is a potent inhibitor of the mitotic kinesin KSP (Eg5), with a Ki of 0.1 nM.

IC50 & Target[1]

Eg5

0.1 nM (Ki)

体外研究
(In Vitro)

SB-743921 is a potent inhibitor of Eg5, with a Ki of 0.1 nM[1]. SB-743921 (1 nM) potently inhibits colony forming cell (CFC) formation of chronic myeloid leukemia (CML) primary cells, but exhibits slight inhibitory activities on the colony-forming ability of normal bone marrow progenitors. SB-743921 (1, 3 nM) induces apoptosis of CML primary CD34 + cells, and shows slight effect on normal CD34 + cells. SB-743921 (2 nM) in combination with imatinib displays additive anti-proliferative effect in KCL22 and CML CD34 + cells. Furthermore, SB-743921 overcomes imatinib resistance in CML cells. SB-743921 (0.5 nM, 1 nM, 3 nM) inhibits MEK/ERK and AKT signaling in CML cells[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)

SB-743921 has good oral bioavailability and pharmacokinetics and induces complete tumor regression in nude mice bearing lung cancer patient xenografts[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.
Clinical Trial

分子量

553.52

Formula

C31H34Cl2N2O3
CAS 号

940929-33-9
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 (180.66 mM)

H2O : 10 mg/mL (18.07 mM; ultrasonic and warming and heat to 60°C)

* “≥” 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 1.8066 mL 9.0331 mL 18.0662 mL
5 mM 0.3613 mL 1.8066 mL 3.6132 mL
10 mM 0.1807 mL 0.9033 mL 1.8066 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：

——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 (4.52 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (4.52 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 (4.52 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (4.52 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 (4.52 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (4.52 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]. Jeffrey R. Jackson, et al. A second generation KSP inhibitor, SB-743921, is a highly potent and active therapeutic in preclinical models of cancer. First AACR International Conference on Molecular Diagnostics in Cancer Therapeutic Development, Sep 12-15, 2006.

    [2]. Yin Y, et al. Kinesin spindle protein inhibitor SB743921 induces mitotic arrest and apoptosis and overcomes imatinib resistance of chronic myeloid leukemia cells. Leuk Lymphoma. 2015 Jun;56(6):1813-20.

    [3]. Good JA, et al. Optimized S-trityl-L-cysteine-based inhibitors of kinesin spindle protein with potent in vivo antitumor activity in lung cancer xenograft models. J Med Chem. 2013 Mar 14;56(5):1878-93.
Cell Assay
[2]

K562 and KCL22 cells are seeded in six-well plates at a number of 5 × 105 in 2 mL RPMI-1640 medium supplemented with 10% FBS in a 5% CO2 atmosphere at 37°C, and are treated with control (2% DMSO), 50 nM imatinib, 2 nM SB-743921 and 50 nM imatinib + 2 nM SB-743921, respectively. Cell number and viability are determined every 24 h. Results are plotted for live cells against time to generate a growth curve[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]

The animal experiments are performed with female NMRI nu/nu mice. Tumor fragments are obtained from xenografts in serial passage in nude mice. Mice are randomized to the various groups, and dosing is started when the required number of mice carries a tumor of 50-250 mm3 volume, preferably 80-200 mm3. Vehicle for 1: 10% ethanol, 10% cremophor, 80% D5W (dextrose 5%); vehicle for all other compounds (including SB-743921): 8% DMSO, 2% Tween 80, distilled water (pH 5). All treatments are given intraperitoneally. Vehicle control mice (group 1) are treated with 10 mL/kg vehicle on days 0, 3, 6, 8, 10, 13, 20, 22, 24, 29, 31, 34, 36, 38, 48, 51, 55, 58, 62, 65, and 69[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]. Jeffrey R. Jackson, et al. A second generation KSP inhibitor, SB-743921, is a highly potent and active therapeutic in preclinical models of cancer. First AACR International Conference on Molecular Diagnostics in Cancer Therapeutic Development, Sep 12-15, 2006.

    [2]. Yin Y, et al. Kinesin spindle protein inhibitor SB743921 induces mitotic arrest and apoptosis and overcomes imatinib resistance of chronic myeloid leukemia cells. Leuk Lymphoma. 2015 Jun;56(6):1813-20.

    [3]. Good JA, et al. Optimized S-trityl-L-cysteine-based inhibitors of kinesin spindle protein with potent in vivo antitumor activity in lung cancer xenograft models. J Med Chem. 2013 Mar 14;56(5):1878-93.

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

Pacritinib(Synonyms: SB1518)

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。

Pacritinib (Synonyms: SB1518) 纯度: 99.75%

Pacritinib (SB1518) 是一种有效的野生型 JAK2 和 JAK2V617F 突变型抑制剂，IC50 分别为 23 nM 和 19 nM。Pacritinib 也抑制 FLT3 及其突变型 FLT3D835Y，IC50 分别为 22 nM 和 6 nM。

Pacritinib(Synonyms: SB1518)

Pacritinib Chemical Structure

CAS No. : 937272-79-2

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 ￥1560 In-stock
2 mg ￥950 In-stock
5 mg ￥1500 In-stock
10 mg ￥2700 In-stock
50 mg ￥12000 In-stock
100 mg ￥21000 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

Pacritinib 相关产品

•相关化合物库:

  • Drug Repurposing Compound Library Plus
  • Clinical Compound Library Plus
  • Bioactive Compound Library Plus
  • Epigenetics Compound Library
  • Immunology/Inflammation Compound Library
  • JAK/STAT Compound Library
  • Kinase Inhibitor Library
  • Protein Tyrosine Kinase Compound Library
  • Stem Cell Signaling Compound Library
  • Anti-Cancer Compound Library
  • Clinical Compound Library
  • Anti-Aging Compound Library
  • Drug Repurposing Compound Library
  • Differentiation Inducing Compound Library
  • Reprogramming Compound Library
  • Macrocyclic Compound Library
  • Anti-Breast Cancer Compound Library
  • Anti-Lung Cancer Compound Library
  • Anti-Pancreatic Cancer Compound Library
  • Anti-Blood Cancer Compound Library
  • Anti-Liver Cancer Compound Library
  • Rare Diseases Drug Library

生物活性

Pacritinib (SB1518) is a potent inhibitor of both wild-type JAK2 (IC50=23 nM) and JAK2V617F mutant (IC50=19 nM). Pacritinib also inhibits FLT3 (IC50=22 nM) and its mutant FLT3D835Y (IC50=6 nM).

IC50 & Target[1]

JAK2V617F

19 nM (IC50)

JAK2wt

23 nM (IC50)

Tyk2

50 nM (IC50)

JAK3

520 nM (IC50)

JAK1

1280 nM (IC50)

FLT3D835Y

6 nM (IC50)

FLT3wt

22 nM (IC50)

体外研究
(In Vitro)

Relative to JAK2, Pacritinib (SB1518) is two-fold less potent against TYK2 (IC50=50 nM), 23-fold less potent against JAK3 (IC50=520 nM) and 56-fold less potent against JAK1 (IC50=1280 nM). The rest of the evaluated kinases show <30% inhibition when tested against 100 nM Pacritinib at adenosine triphosphate concentrations equivalent to its Michaelis constant (Km). Pacritinib inhibits MV4-11 and MOLM-13 cells (both of which are cell lines derived from human acute myeloid leukemias driven by an FLT3 ITD mutation) with IC50 of 47 and 67 nM, respectively. Pacritinib inhibits Karpas 1106P and Ba/F3-JAK2V617F cells (which are cell lines dependent on JAK2 signaling) with IC50 of 348 and 160 nM, respectively[1]. FLT3-ITD harboring MV4-11 cells are treated for 3 h with different concentrations of Pacritinib (SB1518) and pFLT3, pSTAT5 and pERK1/2 levels are quantified. Pacritinib leads to a dose-dependent decrease of pFLT3, pSTAT5, pERK1/2 and pAkt with IC50 of 80, 40, 33 and 29 nM, respectively. The IC50 on auto-phosphorylation of FLT3-wt in RS4;11 is four-fold higher (IC50=600 nM) compare with FLT3-ITD in MV4-11 and MOLM-13 cells. However, STAT5 inhibition is detected at much lower concentrations of Pacritinib (IC50=8 nM)[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)

For evaluation of efficacy in the Ba/F3-JAK2V617F engraftment model, mice are treated with Pacritinib (SB1518) at doses of 50 or 150 mg/kg p.o. q.d. for 13 days, with drug dosing starting 4 days after cell inoculation. At study termination, the vehicle control mice exhibit splenomegaly and hepatomegaly (~7- and 1.3-fold, respectively), reminiscent of the symptoms found in patients with symptomatic myelofibrosis. SB1518 treatment at 150 mg/kg p.o. q.d. significantly ameliorates all these symptoms, with 60% (±9%) normalization of spleen weight and 92% (±5%) normalization of liver weight and is well tolerated without significant weight loss or any hematological toxicities, including thrombocytopenia and anemia[1]. In rats, Pacritinib (SB1518) shows moderately fast absorption (tmax=4 h), with a peak concentration of 114 ng/mL, AUC of 599 ng•h/mL, and a terminal half-life of ~6 h following a single oral dose of 10 mg/kg. In dogs, Pacritinib (SB1518) is rapidly absorbed (tmax=2.0 h), with a peak concentration of ~12 ng/mL, AUC of 53 ng•h/mL, and a terminal half-life of 3.4 h following a single oral dose of 3 mg/kg[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.
Clinical Trial

分子量

472.58

Formula

C28H32N4O3
CAS 号

937272-79-2
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 : 5 mg/mL (10.58 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.1160 mL 10.5802 mL 21.1604 mL
5 mM 0.4232 mL 2.1160 mL 4.2321 mL
10 mM 0.2116 mL 1.0580 mL 2.1160 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: ≥ 1 mg/mL (2.12 mM); Clear solution

    此方案可获得 ≥ 1 mg/mL (2.12 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 (2.12 mM); Suspended solution; Need ultrasonic

    此方案可获得 1 mg/mL (2.12 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 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： 5% DMSO    40% PEG300    5% Tween-80    50% saline

    Solubility: ≥ 0.3 mg/mL (0.63 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]. Hart S, et al. SB1518, a novel macrocyclic pyrimidine-based JAK2 inhibitor for the treatment of myeloid and lymphoid malignancies. Leukemia. 2011 Nov;25(11):1751-9.

    [2]. Hart S, et al. Pacritinib (SB1518), a JAK2/FLT3 inhibitor for the treatment of acute myeloid leukemia. Blood Cancer J. 2011 Nov;1(11):e44.

    [3]. William AD, et al. Discovery of the macrocycle 11-(2-pyrrolidin-1-yl-ethoxy)-14,19-dioxa-5,7,26-triaza-tetracyclo[19.3.1.1(2,6).1(8,12)]heptacosa-1(25),2(26),3,5,8,10,12(27),16,21,23-decaene (SB1518), a potent Janus kinase 2/fms-like tyrosine kinase-3 (JA
Kinase Assay
[1]

All assays are carried out in 384-well white microtiter plates. Compounds (e.g., Pacritinib) are 4-fold serially diluted in 8 steps, starting from 10 µM. The reaction mixture consist of 25 µL assay buffer (50 mM HEPES pH 7.5, 10 mM MgCl2, 5 mM MnCl2, 1 mM DTT, 0.1 mM Na3VO4, 5 mM β-glycerol phosphate). For FLT3 assays, the reaction contain 2.0 µg/mL FLT3 enzyme, 5 µM of poly(Glu,Tyr) substrate and 4 µM of ATP. For JAK1 assays, the reaction contain 2.5 µg/mL of JAK1 enzyme, 10 µM of poly(Glu,Ala,Tyr) substrate and 1.0 µM of ATP. For JAK2 assays, the reaction contain 0.35 µg/mL of JAK2 enzyme, 10 µM of poly (Glu,Ala,Tyr) substrate and 0.15 µM of ATP. For JAK3 assays, the reaction contain 3.5 µg/mL of JAK3 enzyme, 10 µM of poly (Glu,Ala,Tyr) substrate and 6.0 µM of ATP. For TYK2 assays, the reaction contain 2.5 µg/mL of TYK2 enzyme, 10 µM of poly (Glu,Ala,Tyr) substrate and 0.15 µM of ATP. The reaction is incubated at room temperature for 2 h prior to addition of 13 µL PKLight detection reagent. After 10 min incubation luminescent signals are read on a multi-label 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]

SET-2 and Karpas 1106P cells, and Ba/F3-JAK2V617F-GFP-Luc cells are used. For proliferation assays in 96-well plates, cells are seeded at 30-50% confluency and are treated the following day with compounds (e.g., Pacritinib) (in triplicate) at concentrations up to 10 μM for 48 h. Cell viability is monitored using the CellTiter-Glo assay. Dose-response curves are plotted to determine IC50 values for the compounds using the XL-fit software[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][3]

Mice[1]
Female athymic BALB/c nude mice (BALB/cOlaHsd-Foxn1nu) of age 12 weeks are used; and female SCID Beige mice (CB17.Cg-PrkdcscidLystbg/Crl) of age 9-10 weeks are used. For the SET-2 leukemia model, 5×106 tumor cells are injected subcutaneously in the right flank of severe combined immunodeficient beige mice. The cells are resuspended in 50 μL serum-free growth medium, mixed 1:1 with Matrigel and injected in a total volume of 100 μL. Tumor volumes are determined by caliper measurements and drug treatment is initiated after 31 days when tumors have reached a mean volume of 280 mm3 (tumor volume (mm3)=(w2×l)/2). This study is performed using 12 mice per group and animals are killed 3 h post-dose on day 18. Tumor growth inhibition is calculated. For the efficacy studies, mice are treated by oral gavage (10 mL/kg body weight) with doses from 50 to 150 mg/kg SB1518.
Rats and Dogs[3]
Male Wistar rats (aged 6-8 weeks, weighing 270 to 325 g) and male Beagle dogs (6 to 7 months of age, weighing 9-11 kg) are used in this study. The oral doses for dogs and rats are 3, and 10 mg/kg, respectively. The doses are administered, by gavage, as suspensions (0.5 % methylcellulose and 0.1%tween 80) to rats, and as gelatin capsules to dogs. Following oral dosing, serial blood samples are collected (jugular vein in dogs, and superior vena cava in rats) at different time points (0 to 24 h) in tubes containing K3EDTA as anticoagulant, and centrifuged, the plasma is separated and stored at -70°C until analysis. Plasma samples are processed and analyzed by LC/MS/MS. Pharmacokinetic parameters are estimated by noncompartmental methods using WinNonlin.

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]. Hart S, et al. SB1518, a novel macrocyclic pyrimidine-based JAK2 inhibitor for the treatment of myeloid and lymphoid malignancies. Leukemia. 2011 Nov;25(11):1751-9.

    [2]. Hart S, et al. Pacritinib (SB1518), a JAK2/FLT3 inhibitor for the treatment of acute myeloid leukemia. Blood Cancer J. 2011 Nov;1(11):e44.

    [3]. William AD, et al. Discovery of the macrocycle 11-(2-pyrrolidin-1-yl-ethoxy)-14,19-dioxa-5,7,26-triaza-tetracyclo[19.3.1.1(2,6).1(8,12)]heptacosa-1(25),2(26),3,5,8,10,12(27),16,21,23-decaene (SB1518), a potent Janus kinase 2/fms-like tyrosine kinase-3 (JA

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

大鼠S100B蛋白ELISA试剂盒,大鼠(S-100B)BS-8539

发表于由

大鼠S100B蛋白ELISA试剂盒,大鼠(S-100B)

  • 产品型号：BS-8539
  • 简要描述：大鼠S100B蛋白ELISA试剂盒,大鼠(S-100B)ELISAkit上海金畔生物供应ELISA试剂盒种属全，实验室耗材种类全，PCR耗材，离心管，进口吸头等等。
产品咨询在线客服
  • 产品简介

大鼠S100B蛋白ELISA试剂盒,大鼠(S-100B)ELISAkit金畔生物公司供应：ELISA试剂盒,动物血清，荧光定量PCR耗材，移液器吸嘴，微量离心管，进口冻存管，细胞培养皿，培养板，培养瓶，吸头，仪器及手套，色谱耗材，针头过滤器。

产品名称：大鼠S100B蛋白(S-100B)ELISA试剂盒
货号：BS-8539
规格：96T/48T
检测种属：人、大小鼠、豚鼠、兔子、猪、犬、牛羊、鸡鸭、猴ELISA试剂盒等种属。
保存条件及有效期：
1、试剂盒保存：2-8℃。
2、有效期：6个月

大鼠S100B蛋白ELISA试剂盒,大鼠(S-100B)ELISAkit
【测试种属】犬、大小鼠、人、豚鼠、兔子、牛羊、猪、鸡鸭elisa试剂盒等种属
【储存方式】：2-901℃
【检测目的】用于测定血清，血浆及相关液体等样本。例如适合检测包括血清、血浆、尿液、胸腹水、灌洗液、脑脊液、细胞培养上清、组织匀浆等标本。
【用途】科研实验专用，不用于临床诊断。

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大鼠基质金属蛋白酶10ELISA试剂盒,大鼠(MMP-10)ELISAkit
大鼠基质金属蛋白酶13ELISA试剂盒,大鼠(MMP-13)ELISAkit
大鼠基质金属蛋白酶2/明胶酶AELISA试剂盒,大鼠(MMP-2/GelatinaseA)ELISAkit
大鼠基质金属蛋白酶3ELISA试剂盒,大鼠(MMP-3)ELISAkit
大鼠基质金属蛋白酶7ELISA试剂盒,大鼠(MMP-7)ELISAkit
大鼠基质金属蛋白酶8/中性粒细胞胶原酶ELISA试剂盒,大鼠(MMP-8)ELISAkit
大鼠骨保护素ELISA试剂盒,大鼠(OPG)ELISAkit
大鼠B因子ELISA试剂盒,大鼠(BF)ELISAkit
大鼠胎盘生长因子ELISA试剂盒,大鼠(PLGF)ELISAkit
大鼠P选择素ELISA试剂盒,大鼠(P-Selectin/CD62P)ELISAkit
大鼠正常T细胞表达和分泌因子ELISA试剂盒,大鼠(RANTES/CCL5)ELISAkit
大鼠可溶性白细胞分化抗原30配体ELISA试剂盒,大鼠(sCD30L)ELISAkit
大鼠可溶性白细胞分化抗原40配体ELISA试剂盒,大鼠(sCD40L)ELISAkit
大鼠干细胞因子受体ELISA试剂盒,大鼠(SCFR)ELISAkit
大鼠血管生成素受体Tie1ELISA试剂盒,大鼠(ANG-R-Tie1)ELISAkit
大鼠血管生成素受体Tie2ELISA试剂盒,大鼠(ANG-R-Tie2)ELISAkit
大鼠基质金属蛋白酶抑制因子2ELISA试剂盒,大鼠(TIMP-2)ELISAkit
大鼠基质金属蛋白酶抑制因子3ELISA试剂盒,大鼠(TIMP-3)ELISAkit
大鼠基质金属蛋白酶抑制因子4ELISA试剂盒,大鼠(TIMP-4)ELISAkit

产品用途：可用于科研实验！

Adezmapimod hydrochloride(Synonyms: SB 203580 hydrochloride; RWJ 64809 hydrochloride)

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。

Adezmapimod hydrochloride (Synonyms: SB 203580 hydrochloride; RWJ 64809 hydrochloride) 纯度: 99.02%

Adezmapimod (SB 203580) hydrochloride 是一种选择性的，ATP 竞争性的 p38 MAPK 抑制剂，对 SAPK2a/p38 和 SAPK2b/p38β2 的 IC50 分别为 50 nM 和 500 nM。Adezmapimod hydrochloride 抑制 LCK，GSK3β 和 PKBα，IC50 比 SAPK2a/p38 高 100-500 倍。Adezmapimod hydrochloride 是一种自噬 (autophagy) 和有丝分裂 (mitophagy) 激活剂。

Adezmapimod hydrochloride(Synonyms: SB 203580 hydrochloride; RWJ 64809 hydrochloride)

Adezmapimod hydrochloride Chemical Structure

CAS No. : 869185-85-3

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥660 In-stock
10 mg ￥600 In-stock
50 mg ￥1400 In-stock
100 mg ￥2400 In-stock
200 mg ￥3800 In-stock
500 mg   询价  
1 g   询价  

* Please select Quantity before adding items.

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生物活性

Adezmapimod (SB 203580) hydrochloride is a selective and ATP-competitive p38 MAPK inhibitor with IC50s of 50 nM and 500 nM for SAPK2a/p38 and SAPK2b/p38β2, respectively. Adezmapimod hydrochloride inhibits LCK, GSK3β and PKBα with IC50s of 100-500-fold higher than that for SAPK2a/p38. Adezmapimod hydrochloride is an autophagy and mitophagy activator[1].

IC50 & Target[1]

p38

50 nM (IC50)

p38β2

500 nM (IC50)

体外研究
(In Vitro)

Adezmapimod hydrochloride (preincubated with 0-30 μM for 1 h and cultured for 24 h in the presence of 20 ng/mL IL-2) prevents the IL-2-induced proliferation of primary human T cells, murine CT6 T cells, or BAF F7 B cells with an IC50 of 3-5 μM[1].
Adezmapimod hydrochloride blocks PKB phosphorylation (IC50 3-5 μM). Adezmapimod hydrochloride inhibitsthe phosphorylation of Ser473 in a dose-dependent manner in both CT6 and activated human T cells and IL-2-responsive BA/F3 F7 B cells[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 Proliferation Assay[1]

Cell Line: CT6, BA/F3 cell line F7, and PBMC/T cells
Concentration: 0-30 μM
Incubation Time: Preincubated with 0-30 μM SB203580 for 1 h and cultured for 24 h in the presence of 20 ng/mL IL-2
Result: Prevented the IL-2-induced proliferation of primary human T cells, murine CT6 T cells, or BAF F7 B cells with an IC50 of 3-5 μM.

Western Blot Analysis[1]

Cell Line: CT6 cells, activated human T cells, and BA/F3 F7 cells
Concentration: 0-30 μM
Incubation Time: Preincubated with 0-30 μM SB203580 for 1 h before stimulating with 20 ng/mL IL-2 for 5 min
Result: Inhibited the phosphorylation of PKB at Ser473 in a dose-dependent manner.

体内研究
(In Vivo)

Adezmapimod hydrochloride (5 mg/kg/day; intra peritoneal injected daily for 16 consecutive days, in female atymic Nu/Nu mice) treatment, p38WT tumors show a significantly smaller tumor burden when compared with p38TM tumors that were treated in parallel[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 Model: Six-week-old female atymic Nu/Nu mice CAL27 p38WT and p38TM tumors[1]
Dosage: 5 mg/kg/day
Administration: Intra peritoneal injected daily for 16 consecutive days
Result: After 2 weeks treatment, CAL27 p38WT tumors were significantly smaller; CAL27 p38TM tumors were not affected by the p38 inhibitor (n=10).  

分子量

413.90

Formula

C21H17ClFN3OS
CAS 号

869185-85-3
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 (241.60 mM; Need ultrasonic)

H2O : 8.43 mg/mL (20.37 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 2.4160 mL 12.0802 mL 24.1604 mL
5 mM 0.4832 mL 2.4160 mL 4.8321 mL
10 mM 0.2416 mL 1.2080 mL 2.4160 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：

——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 (6.04 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (6.04 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% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (6.04 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (6.04 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 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]. Davies SP, et al. Specificity and mechanism of action of some commonly used protein kinase inhibitors. Biochem J. 2000 Oct 1;351(Pt 1):95-105.

    [2]. Lali FV, et al. The pyridinyl imidazole inhibitor SB203580 blocks phosphoinositide-dependent protein kinase activity, protein kinase B phosphorylation, and retinoblastoma hyperphosphorylation in interleukin-2-stimulated T cells independently of p38 mitogen-activated protein kinase. J Biol Chem. 2000 Mar 10;275(10):7395-402.

    [3]. Leelahavanichkul K, et al. A role for p38 MAPK in head and neck cancer cell growth and tumor-induced angiogenesis and lymphangiogenesis. Mol Oncol. 2014 Feb;8(1):105-18.

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

Eltrombopag(Synonyms: 艾曲波帕; SB-497115)

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。

Eltrombopag (Synonyms: 艾曲波帕; SB-497115) 纯度: 99.82%

Eltrombopag (SB-497115) 是一种血小板生成素 (TPO) 受体激动剂，用于血小板减少的某些病症研究。

Eltrombopag(Synonyms: 艾曲波帕; SB-497115)

Eltrombopag Chemical Structure

CAS No. : 496775-61-2

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 ￥858 In-stock
10 mg ￥780 In-stock
50 mg ￥2350 In-stock
100 mg ￥2800 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

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生物活性

Eltrombopag (SB-497115) is a thrombopoietin (TPO) receptor agonist developed for certain conditions that lead to thrombocytopenia.

Clinical Trial

分子量

442.47

Formula

C25H22N4O4
CAS 号

496775-61-2
中文名称

艾曲波帕；伊屈泼帕
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 : 8.33 mg/mL (18.83 mM; Need ultrasonic)

H2O : < 0.1 mg/mL (insoluble)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.2600 mL 11.3002 mL 22.6004 mL
5 mM 0.4520 mL 2.2600 mL 4.5201 mL
10 mM 0.2260 mL 1.1300 mL 2.2600 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: ≥ 1 mg/mL (2.26 mM); Clear solution

    此方案可获得 ≥ 1 mg/mL (2.26 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

*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]. Erickson-Miller CL, et al. Preclinical activity of eltrombopag (SB-497115), an oral, nonpeptide thrombopoietin receptor agonist. Stem Cells. 2009 Feb;27(2):424-30.

    [2]. Erickson-Miller CL, et al. Discovery and characterization of a selective, nonpeptidyl thrombopoietin receptor agonist. Exp Hematol. 2005 Jan;33(1):85-93.

    [3]. McHutchison JG, et al. Eltrombopag for thrombocytopenia in patients with cirrhosis associated with hepatitis C. N Engl J Med. 2007 Nov 29;357(22):2227-36.

    [4]. Jenkins JM, et al. Phase 1 clinical study of eltrombopag, an oral, nonpeptide thrombopoietin receptor agonist. Blood. 2007 Jun 1;109(11):4739-41.

    [5]. Saleh MN, et al. Safety and efficacy of eltrombopag for treatment of chronic immune thrombocytopenia: results of the long-term, open-label EXTEND study. Blood. 2013 Jan 17;121(3):537-45.

    [6]. Juan Zhu, et al. Identification of Eltrombopag as a Repurposing Drug Against Staphylococcus epidermidis and its Biofilms. Curr Microbiol. 2021 Feb 21.

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

SB-505124

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。

SB-505124  纯度: 99.63%

SB-505124 是一种选择性的 TGF-βI 型受体 (ALK4，ALK5，ALK7) 抑制剂，对 ALK4，ALK5 的 IC50 值分别为 129 nM 和 47 nM，对 ALK1，2，3 或 6 无作用。

SB-505124

SB-505124 Chemical Structure

CAS No. : 694433-59-5

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 ￥1228 In-stock
10 mg ￥1116 In-stock
50 mg ￥3906 In-stock
100 mg   询价  
200 mg   询价  

* Please select Quantity before adding items.

SB-505124 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus
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  • Reprogramming Compound Library
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  • Angiogenesis Related Compound Library
  • Anti-Colorectal Cancer Compound Library

生物活性

SB-505124 is a selective inhibitor of TGF-β Receptor type I receptors (ALK4, ALK5, ALK7), with IC50s of 129 nM and 47 nM for ALK4, ALK5, respectively, but it does not inhibit ALK1, 2, 3, or 6.

IC50 & Target

IC50: 129 nM (ALK4), 47 nM (ALK5)
体外研究
(In Vitro)

SB-505124 demonstrates no toxicity to renal epithelial A498 cells at concentrations up to 100 μM for 48 h. 505124 inhibits the closely related ALK4 with an IC50 value of 129±11 nM (about 2.5-fold less sensitive than ALK5) but does not inhibit ALK2 at concentrations up to 10 μM. SB-505124 (1 μM) inhibits the TGF-β-induced phosphorylation of Smad2 in all three of these cell lines in a concentration-dependent fashion. SB-505124 (1 or 5 μM) potently inhibits TGF-β-induced activation of JNK/SAP, extracellular signal-regulated kinase 1/2, and p38 despite the different patterns of activation in these cells[1]. SB-505124 (10 µM) impairs Smad2 phosphorylation and CTGF and α-SMA expression in vitro[2]. SB-505124 susspresses CTGF and α-SMA observed by immunofluorescence. Cell outgrowth from explants dissected from eyes to which SB-505124 is applied during GFS is robust while outgrowth is poor from those treated with MMC[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)

SB-505124 (5 mg/kg; i.p.) alone has no effect in C57Bl6 mice with A549 xenografts, but administration of SB-505124 with a single dose of Carboplatin (60 mg/kg) results in durable responses without the need for maintenance therapy in five animals[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.

Animal Model: C57Bl6 mice with A549 xenografts[4]
Dosage: 5 mg/kg
Administration: I.p.; daily
Result: Had no effect alone, but administration with a single dose of carboplatin (60 mg/kg) resulted in durable responses without the need for maintenance therapy in five animals.

分子量

335.40

Formula

C20H21N3O2
CAS 号

694433-59-5
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 : 113.33 mg/mL (337.90 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.9815 mL 14.9076 mL 29.8151 mL
5 mM 0.5963 mL 2.9815 mL 5.9630 mL
10 mM 0.2982 mL 1.4908 mL 2.9815 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 (7.45 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (7.45 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 (7.45 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (7.45 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]. DaCosta Byfield S, et al. SB-505124 is a selective inhibitor of transforming growth factor-beta type I receptors ALK4, ALK5, and ALK7. Mol Pharmacol. 2004 Mar;65(3):744-52.

    [2]. Sutariya V, et al. reversible gel for delivery of receptor-like kinase 5 inhibitor SB-505124 for glaucoma filtration surgery. Pharm Dev Technol. 2013 Jul-Aug;18(4):957-62.

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