252003-71-7
中文名稱
CP-547632 (hydrochloride)
英文名稱
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 結(jié)構(gòu)式
物理化學(xué)性質(zhì)
儲存條件-20°C儲存
溶解度DMSO: 38.33 mg/mL (67.38 mM); Water: < 0.1 mg/mL (insoluble)
形態(tài)Solid
顏色White to light yellow
CP-547632 (hydrochloride)價格(試劑級)
| 報價日期 | 產(chǎn)品編號 | 產(chǎn)品名稱 | CAS號 | 包裝 | 價格 |
| 2024/11/08 | HY-13302B | CP-547632 (hydrochloride) CP-547632 hydrochloride | 252003-71-7 | 5mg | 850元 |
| 2024/11/08 | HY-13302B | CP-547632 (hydrochloride) CP-547632 hydrochloride | 252003-71-7 | 10mM * 1mLin DMSO | 1060元 |
| 2024/11/08 | HY-13302B | CP-547632 (hydrochloride) CP-547632 hydrochloride | 252003-71-7 | 10mg | 1250元 |
常見問題列表
生物活性
CP-547632 hydrochloride 是一種口服有效的，ATP 競爭性的 VEGFR-2 和 FGF 激酶抑制劑，IC50 分別為 11 nM 和 9 nM。CP-547632 hydrochloride 對 VEGFR2 和 bFGF 的選擇性高于 EGFR，PDGFRβ 和相關(guān)的酪氨酸激酶 (TKs)。CP-547632 hydrochloride 具有抗腫瘤作用。靶點
|
VEGFR-2 11 nM (IC 50 ) |
FGFR 9 nM (IC 50 ) |
體外研究
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. |
體內(nèi)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. |