CP-547632TFA是一种口服有效的，ATP竞争性的VEGFR-2和FGF激酶抑制剂，IC50分别为11nM和9nM。CP-547632TFA对VEGFR2和bFGF的选择性高于EGFR，PDGFRβ和相关的酪氨酸激酶(TKs)。CP-547632TFA具有抗肿瘤作用。
货号:ajcx30436
CAS:N/A
分子式:C22H25BrF5N5O5S
分子量：646.43
溶解度:DMSO: 150 mg/mL (232.04 mM)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

CP-547632 TFA is an orally active, ATP-competitive and potent VEGFR-2 and FGF kinases inhibitor with IC50s of 11 nM and 9 nM, respectively. CP-547632 TFA is selective for VEGFR2 and bFGF over EGFR, PDGFRβ, and related tyrosine kinases (TKs). CP-547632 TFA has antitumor efficacy[1].

CP-547632 TFA (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 TFA (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 TFA (oral; 50 mg/kg; a single oral dose) yieldes plasma concentrations above 500 ng/ml for 12 hours[1]. Animal Model: Athymic female mice (CD-1 nu/nu) 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.