产品
编 号:F293342
分子式:C20H25BrClF2N5O3S
分子量:568.86
产品类型
结构图
CAS No: 252003-71-7
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产品详情
生物活性:
CP-547632 hydrochloride 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 hydrochloride is selective for VEGFR2 and bFGF over EGFR, PDGFRβ, and related tyrosine kinases (TKs). CP-547632 hydrochloride has antitumor efficacy.
体内研究:
CP-547632 hydrochloride (口服;6.25-100 mg/kg/天;持续 10-24 天) 对 Colo -205、DLD-1 和 MDA-MB-231 异种移植物的生长产生剂量依赖性抑制。 CP-547632 hydrochloride (口服;50 mg/kg;单次口服剂量) 在 12 小时内产生高于 500 ng/mL 的血浆浓度。Animal Model:Mice bearing tumors (75-150 mm in size)
Dosage:6.25, 12.5, 25, 50, 100 mg/kg
Administration:P.o.; daily; 10-24 days
Result:Caused a dose-dependent inhibition of growth in Colo-205, DLD-1, and MDA-MB-231 xenografts.
Animal Model:H-ras tumor-bearing mice
Dosage:50 mg/kg
Administration:Oral
Result:A single oral dose of 50 mg/kg yielded plasma concentrations above 500 ng/ml for 12 hours.
体外研究:
CP-547632 hydrochloride (1-1000 nM;1 小时) 以剂量依赖性方式抑制 VEGF 刺激的 VEGFR-2 磷酸化,IC50 值为 6 nM。