Vatalanib dihydrochloride,2121

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抑制剂描述：

产品名称：Vatalanib 2HCl

产品别名：见爱必信官网

英文别名：Vatalanib 2HCl

靶点：VEGFR

CAS：212141-51-0

纯度：99%

外观：见爱必信官网

保存方法：Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.

描述：

Vatalanib (PTK787; ZK-222584; CGP-79787)是VEGFR2/KDR抑制剂，IC50为37 nM，对VEGFR1/Flt-1和VEGFR3/Flt-4抑制性较弱。

溶解性：DMSO : 50 mg/mL (119.12 mM; ultrasonic and warming and heat to 80°C)

体外研究：

Vatalanib also inhibits Flk, c-Kit and PDGFRβ with IC50 of 270 nM, 730 nM and 580 nM, respectively. Furthermore, Vatalanib shows the anti-proliferation effect by inhibiting thymidine incorporation induced by VEGF in HUVECs with and IC50 of 7.1 nM, and dose-dependently suppresses VEGF-induced survival and migration of endothelial cells in the same dose range without cytotoxic or antiproliferative effect on cells that do not express VEGF receptors. A recent study shows that Vatalanib significantly inhibits the growth of hepatocellular carcinoma cells and enhances the IFN/5-FU induced apoptosis by increasing proteins levels of Bax and reduced Bcl-xL and Bcl-2.

体内研究：Vatalanib induces dose-dependent inhibition of the angiogenic response to VEGF and PDGF in both a growth factor implant model and a tumor cell-driven angiogenesis model after once-daily oral dosing (25-100 mg/kg). In the same dose range, Vatalanib also inhibits the growth and metastasesof several human carcinomas in nude mice without significant effect on circulating blood cells or bone marrow leukocytes.

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