CP-547632 hydrochloride |
| Catalog No.GC38575 |
Le chlorhydrate de CP-547632 est un inhibiteur des VEGFR-2 et FGF kinases actif par voie orale, compétitif pour l'ATP et puissant avec des CI50 de 11 nM et 9 nM, respectivement. Le chlorhydrate de CP-547632 est sélectif pour le VEGFR2 et le bFGF par rapport À l'EGFR, le PDGFRβ et les tyrosine kinases (TK) apparentées. Le chlorhydrate de CP-547632 a une efficacité antitumorale.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 252003-71-7
Sample solution is provided at 25 µL, 10mM.
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CP-547632 hydrochloride is a well-tolerated, orally-bioavailable inhibitor of the VEGFR-2 and basic fibroblast growth factor (FGF) kinases with IC50s of 11 nM and 9 nM, respectively. CP-547632 hydrochloride is an ATP-competitive kinase inhibitor and it is selective relative to epidermal growth factor receptor, platelet-derived growth factor β, and other related TKs. CP-547632 hydrochloride has antitumor efficacy[1].
CP-547632 hydrochloride (1-1000 nM; 1 hours) inhibits VEGF-stimulated VEGFR-2 phosphorylation in a dose-dependent fashion, with an IC50 value of 6 nM[1]. Western Blot Analysis[1] Cell Line: Serum-deprived cells
CP-547632 hydrochloride (p.o.; 6.25-100 mg/kg/day; for 10-24 days) causes a dose-dependent inhibition of growth in Colo-205, DLD-1, and MDA-MB-231 xenografts[1]. CP-547632 hydrochloride (oral; 50 mg/kg) of a single oral dose of 50 mg/kg yieldes plasma concentrations above 500 ng/ml for 12 hours[1]. Animal Model: Mice bearing tumors (75-150 mm in size)[1]
[1]. Beebe JS, et al. Pharmacological characterization of CP-547,632, a novel vascular endothelial growth factor receptor-2 tyrosine kinase inhibitor for cancer therapy. Cancer Res. 2003 Nov 1;63(21):7301-9.
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