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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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