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保存条件 :Please store the product under the recommended conditions in the Certificate of Analysis.
英文名 :PTK787; ZK-222584; CGP-79787
库存 :货期:电询
供应商 :MedChemExpress LLC
规格 :电询
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Vatalanib
CAS No. : 212141-54-3
MCE 国际站:Vatalanib
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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