CP-547632 (hydrochloride)
| 中文名称 | CP-547632 (hydrochloride) |
|---|---|
| 中文同义词 | 化合物 T10870;CP-547632盐酸盐 |
| 英文名称 | CP-547632 (hydrochloride) |
| 英文同义词 | CP-547632 hydrochloride >=98% (HPLC);CP-547632 HYDROCHLORIDE;CP-547632 hydrochloride (PAN-90806);CP 547632 hydrochloride,CP547632 hydrochloride |
| CAS号 | 252003-71-7 |
| 分子式 | C20H25BrClF2N5O3S |
| 分子量 | 568.86 |
| EINECS号 | |
| 相关类别 | |
| Mol文件 | 252003-71-7.mol |
| 结构式 |  |
CP-547632 (hydrochloride) 性质
| 储存条件 | Store at -20°C |
|---|---|
| 溶解度 | 二甲基亚砜：38.33mg/mL（67.38mM）；水：< 0.1 mg/mL（不溶） |
| 形态 | 固体 |
| 颜色 | 白色至浅黄色 |
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。
|
VEGFR-2 11 nM (IC 50 ) |
FGFR 9 nM (IC 50 ) |
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. |
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. |
安全信息
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2024/04/30 | HY-13302B | CP-547632 (hydrochloride) CP-547632 hydrochloride | 252003-71-7 | 10mM * 1mLin DMSO | 1060元 |
| 2024/04/30 | HY-13302B | CP-547632 (hydrochloride) CP-547632 hydrochloride | 252003-71-7 | 10mg | 1250元 |