Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Telatinib (Bay 57-9352) 是一种口服具有活力的,小分子的 VEGFR2,VEGFR3,PDGFα 和 c-Kit 抑制剂,它们的 IC50 值分别为6,4,15,1 nM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 263 | 现货 | ||
2 mg | ¥ 383 | 现货 | ||
5 mg | ¥ 663 | 现货 | ||
10 mg | ¥ 957 | 现货 | ||
25 mg | ¥ 1,990 | 现货 | ||
50 mg | ¥ 2,990 | 现货 | ||
100 mg | ¥ 4,160 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 728 | 现货 |
产品描述 | Telatinib (Bay 57-9352) is an effective inhibitor of VEGFR2/3, c-Kit, and PDGFRα. The IC50s of Telatinib forVEGFR2/3, c-Kit and PDGFRα are 6 nM/4 nM, 1 nM, and 15 nM, respectively. |
靶点活性 | c-Kit:1 nM, PDGFRα:15 nM, VEGFR3:4 nM, VEGFR2:6 nM |
体外活性 | Telatinib has 0.66, 0.17, and 2.5 times higher IC50 values for VEGFR3, c-Kit, and PDGFRβ than VEGFR2, respectively, while Vatalanib exhibits 18, 20, and 16 times higher IC50 values, respectively, indicating that Telatinib has potential benefit over Vatalanib. Telatinib inhibits VEGFR2 autophosphorylation in a whole-cell assay with an IC50 of 19 nM, suppresses VEGF-dependent proliferation of human umbilical vein endothelial cells with an IC50 of 26 nM, and blocks PDGF-stimulated growth of human aortic smooth muscle cells with an IC50 of 249 nM. [3] Telatinib displays little inhibitory activity against the Raf kinase pathway, epidermal growth factor receptor family, the fibroblast growth factor receptor (FGFR) family, and the Tie-2 receptor. [4] |
体内活性 | Given that tumor development and metastasis are ascribed to deregulated VEGFR signal pathway, Telatinib treatment significantly inhibits tumor growth and metastasis by blocking the VEGFR signaling and subsequently tumor angiogenesis. In addition to the significant inhibition of tumor angiogenesis, Telatinib treatment induces a significant decrease in endothelium-dependent and endothelium-independent vasodilation, as well as reduction in capillary density, leading to an increase in systolic and diastolic blood pressure. [1] Administration of Telatinib as a single agent exhibits a potent anti-tumor activity in multiple human tumor xenograft models including MDA-MB-231 breast cancer, Colo-205 colon cancer, DLD-1 colon cancer, and H460 non-small cell lung cancer, as well as pancreatic and prostate carcinoma in a dose-dependent manner. [2] |
别名 | Bay 57-9352, 替拉替尼 |
分子量 | 409.83 |
分子式 | C20H16ClN5O3 |
CAS No. | 332012-40-5 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
H2O: < 1 mg/mL (insoluble or slightly soluble)
Ethanol: 1 mg/mL (2.44 mM)
DMSO: 76 mg/mL (185.4 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
Ethanol / DMSO | 1 mM | 2.44 mL | 12.2002 mL | 24.4004 mL | 61.0009 mL |
DMSO | 5 mM | 0.488 mL | 2.44 mL | 4.8801 mL | 12.2002 mL |
10 mM | 0.244 mL | 1.22 mL | 2.44 mL | 6.1001 mL | |
20 mM | 0.122 mL | 0.61 mL | 1.22 mL | 3.05 mL | |
50 mM | 0.0488 mL | 0.244 mL | 0.488 mL | 1.22 mL | |
100 mM | 0.0244 mL | 0.122 mL | 0.244 mL | 0.61 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。
Telatinib 332012-40-5 Angiogenesis Tyrosine Kinase/Adaptors c-Kit PDGFR VEGFR CD117 Inhibitor Bay 57-9352 Platelet-derived growth factor receptor 替拉替尼 inhibit Vascular endothelial growth factor receptor SCFR inhibitor