Vatalanib dihydrochlorideCAS号: 212141-51-0分子式: C20H15ClN4·2HCl分子量: 419.73描述纯度储存/保存方法别名可溶性/溶解性靶点In vitro(体外研究)In vivo(体内研究)
产品描述 | |
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。 |
纯度 |
99%
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储存/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.
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基本信息 | |
别名 |
瓦他拉尼二盐酸盐;Vatalanib dihydrochloride;PTK787 dihydrochloride;CGP-797870 dihydrochloride;ZK-222584 dihydrochloride
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可溶性/溶解性 |
DMSO : 50 mg/mL (119.12 mM; ultrasonic and warming and heat to 80°C)
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生物活性 | |
靶点 |
VEGFR2/KDR;VEGFR1/FLT1;VEGFR2/Flk1;PDGFRβ;VEGFR3/FLT4
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In vitro(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.
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In vivo(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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分子结构图