SKU : MC540071
CAS Number : 212141-51-0
Molecular Formula : C20H15ClN4 | Molecular Weight : 346.81
Synonyms : PTK787 dihydrochloride;CGP-797870 dihydrochloride;ZK-222584 dihydrochloride
Quote RequestPurity | NLT 98% |
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Storage | at 20ºC 2 years |
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Chemical Name | Vatalanib (dihydrochloride) |
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CAS Number | 212141-51-0 |
MDL Number | MFCD08458963 |
Molecular Formula | C20H15ClN4 |
Molecular Weight | 346.81 |
Synonyms | PTK787 dihydrochloride;CGP-797870 dihydrochloride;ZK-222584 dihydrochloride |
Vatalanib dihydrochloride (PTK787 dihydrochloride) is an inhibitor of VEGFR2/KDR with IC50 of 37 nM. IC50 & Target: IC50: 37 nM (VEGFR2/KDR)[1] 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[1]. 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[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[1].
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