CP-547632 hydrochloride 是一种耐受良好，口服生物可利用的 VEGFR-2 和碱性成纤维细胞生长因子 (FGF) 激酶抑制剂，IC50 分别为 11 nM 和 9 nM。CP-547632 hydrochloride 是 ATP 竞争性激酶抑制剂，相对于表皮生长因子受体，血小板衍生生长因子 β 和其他相关 TK 具有选择性。CP-547632 hydrochloride 有抗肿瘤功效。
货号:ajcx14996
CAS:252003-71-7
分子式:C20H25BrClF2N5O3S
分子量：568.86
溶解度:DMSO: 38.33 mg/mL (67.38 mM); H2O:< 0.1 mg/mL (insoluble)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

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.