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252003-71-7

中文名称 CP-547632 (hydrochloride)
英文名称 CP-547632 (hydrochloride)
CAS 252003-71-7
分子式 C20H25BrClF2N5O3S
分子量 568.86
MOL 文件 252003-71-7.mol
252003-71-7 结构式 252003-71-7 结构式

基本信息

中文别名
化合物 T10870
英文别名
CP-547632 HYDROCHLORIDE
CP-547632 hydrochloride >=98% (HPLC)

物理化学性质

储存条件-20°C储存
溶解度DMSO: 38.33 mg/mL (67.38 mM); Water: < 0.1 mg/mL (insoluble)
形态Solid
颜色White to light yellow

安全数据

危险性符号(GHS)GHS hazard pictograms
GHS07
警示词警告
危险性描述H315-H319-H335
防范说明P305+P351+P338
CP-547632 (hydrochloride)价格(试剂级)
报价日期产品编号产品名称CAS号包装价格
2024/11/08HY-13302BCP-547632 (hydrochloride)
CP-547632 hydrochloride
252003-71-75mg850元
2024/11/08HY-13302BCP-547632 (hydrochloride)
CP-547632 hydrochloride
252003-71-710mM * 1mLin DMSO1060元
2024/11/08HY-13302BCP-547632 (hydrochloride)
CP-547632 hydrochloride
252003-71-710mg1250元

常见问题列表

生物活性
CP-547632 hydrochloride 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 11 nM 和 9 nM。CP-547632 hydrochloride 对 VEGFR2 和 bFGF 的选择性高于 EGFR,PDGFRβ 和相关的酪氨酸激酶 (TKs)。CP-547632 hydrochloride 具有抗肿瘤作用。
靶点

VEGFR-2

11 nM (IC 50 )

FGFR

9 nM (IC 50 )

体外研究

CP-547632 hydrochloride (1-1000 nM; 1 hours) inhibits VEGF-stimulated VEGFR-2 phosphorylation in a dose-dependent fashion, with an IC 50 value of 6 nM.

Western Blot Analysis

Cell Line: Serum-deprived cells
Concentration: 1, 4, 16, 63, 250, 1000 nM
Incubation Time: 1 hours
Result: Inhibited VEGF-stimulated VEGFR-2 phosphorylation in a dose-dependent fashion.
体内研究

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.
CP-547632 hydrochloride (oral; 50 mg/kg; a single oral dose) yieldes plasma concentrations above 500 ng/ml for 12 hours.

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.
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