Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Vactosertib (EW-7197) 是有效的、具有 ATP 竞争性的、具有口服活性的激活素受体样激酶 5 (ALK5) 抑制剂(IC50:12.9 nM)。它还以纳摩尔浓度抑制 ALK2 和 ALK4 (IC50为 17.3 nM),表现出强大的抗转移活性和抗癌作用。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 278 | 现货 | ||
2 mg | ¥ 393 | 现货 | ||
5 mg | ¥ 659 | 现货 | ||
10 mg | ¥ 947 | 现货 | ||
25 mg | ¥ 1,660 | 现货 | ||
50 mg | ¥ 2,570 | 现货 | ||
100 mg | ¥ 3,990 | 现货 | ||
200 mg | ¥ 5,680 | 现货 | ||
500 mg | ¥ 8,490 | 现货 | ||
1 g | ¥ 11,300 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 728 | 现货 |
产品描述 | Vactosertib (EW-7197) is an orally bioavailable inhibitor of the serine/threonine kinase, transforming growth factor (TGF)-beta receptor type 1 (TGFBR1), also known as activin receptor-like kinase 5 (ALK5), with potential antineoplastic activity. |
靶点活性 | ALK5:11 nM, ALK4:13 nM |
体外活性 | In HaCaT (3TP-luc) and 4T1 (3TP-luc) stable cells, 12b potently inhibits the TGF-β1-induced luciferase reporter activity with IC50 of 16.5 and 12.1 nM, respectively. [1] EW-7197 inhibits TGFβ-induced Smad2 or Smad3 phosphorylation and the epithelial-to-mesenchymal transition (EMT) in TGFβ-treated breast cancer cells. In addition, EW-7197 also abrogates TGFβ1-induced tumor cell migration and invasion in breast cells. [3] |
体内活性 | In rats, EW-7197 shows an oral bioavailability of 51% with high systemic exposure (AUC) of 1426 ng×h/mL and maximum plasma concentration (Cmax) of 1620 ng/mL. EW-7197 also shows low toxicity on the cardiovascular system, central nervous system, and respiratory system. [1] In a mouse B16 melanoma model, EW-7197 (2.5 mg/kg daily p.o.) suppresses the progression of melanoma with enhanced cytotoxic T-lymphocyte (CTL) responses. [2] EW-7197 enhances cytotoxic T lymphocyte activity in 4T1 orthotopic-grafted mice and increased the survival time of 4T1-Luc and 4T1 breast tumor-bearing mice. [3] |
激酶实验 | Protein Kinase Assay: A radioisotopic protein kinase assay (HotSpot assay) is performed at Reaction Biology Corporation. |
细胞实验 | Cells are seeded in 96 well plate and treated with indicated concentrations of EW-7197 in 0.2% HI-FBS medium for 72 h. Cells are dried after incubation with 10% TCA in media. Then, cells are incubated with 0.4% SRB (Sulforhodamine B) in 1% acetic acid for 30 min. After washing with 1% glacial acetic acid, bounded dye is released in 10 mM Tris buffer (pH 10.5) for 30 min. Absorbance is measured at 570 nm. (Only for Reference) |
别名 | TEW-7197, EW-7197 |
分子量 | 399.42 |
分子式 | C22H18FN7 |
CAS No. | 1352608-82-2 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
H2O: < 1 mg/mL (insoluble or slightly soluble)
Ethanol: 40 mg/mL (100.1 mM)
DMSO: 73 mg/mL (182.8 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
Ethanol / DMSO | 1 mM | 2.5036 mL | 12.5182 mL | 25.0363 mL | 62.5908 mL |
5 mM | 0.5007 mL | 2.5036 mL | 5.0073 mL | 12.5182 mL | |
10 mM | 0.2504 mL | 1.2518 mL | 2.5036 mL | 6.2591 mL | |
20 mM | 0.1252 mL | 0.6259 mL | 1.2518 mL | 3.1295 mL | |
50 mM | 0.0501 mL | 0.2504 mL | 0.5007 mL | 1.2518 mL | |
100 mM | 0.025 mL | 0.1252 mL | 0.2504 mL | 0.6259 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
Vactosertib 1352608-82-2 Angiogenesis Stem Cells Tyrosine Kinase/Adaptors ALK TGF-beta/Smad antimetastatic invasion Smad Transforming growth factor beta receptors TGFβ TEW 7197 migration TGF-β Receptor breast TEW-7197 inhibit cell EW7197 TEW7197 cancer survival EW 7197 EW-7197 Inhibitor p38α inhibitor