Vatalanib

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

一种有效的口服 III 类受体酪氨酸激酶抑制剂，对 VEGFR、Flt-1、KDR 和 PDGFRβ 的 IC50 小于 1 uM。

A potent, orally available class III receptor tyrosine kinases inhibitor with IC50 of <1 uM for VEGFR, Flt-1, KDR and PDGFRβ; shows no activity against EGFR, FGFR-1, c-Met, and Tie-2, or c-Src, c-Abl, and PKC-α; blocks the VEGF-induced receptor autophosphorylation in CHO cells ectopically expressing the KDR receptor with IC50 of 34 nM; inhibits EGF and PDGF-induced angiogenesis in a growth factor implant model (25-100 mg/kg).Ovarian Cancer Phase 1 Discontinued(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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PTK787 | PTK/ZK | CGP-79787D | CGP-79787 | ZK-222584

Angiogenesis

VEGFR

PDGFRβ|VEGFR1/FLT1|VEGFR2/Flk1|VEGFR2/KDR|VEGFR3/FLT4

Cancer

Ovarian Cancer

212141-51-0

419.7348

C20H17Cl3N4

>98% (HPLC)

10 mM in DMSO

ClC1=CC=C(NC2=NN=C(CC3=CC=NC=C3)C4=C2C=CC=C4)C=C1.[H]Cl.[H]Cl

1-Phthalazinamine, N-(4-chlorophenyl)-4-(4-pyridinylmethyl)-, hydrochloride (1:2)

(-20℃)

With Ice Pack

≥ 2 years