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Vatalanib free base

CAS No. : 212141-54-3

MCE 站：Vatalanib free base

产品活性：Vatalanib（PTK787; ZK-222584; CGP-79787）是VEGFR2/KDR的抑制剂，其IC₅₀值为37nM。

研究领域：Protein Tyrosine Kinase/RTK

作用靶点：VEGFR

In Vitro: Vatalanib also inhibits Flk, c-Kit and PDGFRβ with IC₅₀ of 270 nM, 730 nM and 580 nM, respectively. 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.

In Vivo: 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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