252003-65-9
中文名稱
3-[(4-溴-2,6-二氟芐基)氧基]-5-[3-[4-(吡咯烷-1-基)丁基]脲基]異噻唑-4-甲酰胺
英文名稱
CP-547632
CAS
252003-65-9
分子式
C20H24BrF2N5O3S
分子量
532.4
MOL 文件
252003-65-9.mol
更新日期
2024/05/13 15:47:52
252003-65-9 結(jié)構(gòu)式
基本信息
中文別名
3-[(4-溴-2,6-二氟芐基)氧基]-5-[3-[4-(吡咯烷-1-基)丁基]脲基]異噻唑-4-甲酰胺 英文別名
CS-1957CP-547632
CP-547632(CP 547632)
3-((4-Bromo-2,6-difluorobenzyl)oxy)-5-(3-(4-(pyrrolidin-1-yl)butyl)ureido)isothiazole-4-carbox
3-((4-Bromo-2,6-difluorobenzyl)oxy)-5-(3-(4-(pyrrolidin-1-yl)butyl)ureido)isothiazole-4-carboxami
3-[(4-Bromo-2,6-difluorobenzyl)oxy]-5-[3-[4-(pyrrolidin-1-yl)butyl]ureido]isothiazole-4-carboxamide
3-(4-Bromo-2,6-difluorobenzyloxy)-5-(3-(4-pyrrolidin-1-ylbutyl)ureido)isothiazole-4-carboxylic acid amide
3-[(4-broMo-2,6-difluorophenyl)Methoxy]-5-[[[[4-(1-pyrrolidinyl)butyl]aMino]carbonyl]aMino]-4-isothiazolecarboxaMide
4-Isothiazolecarboxamide, 3-((4-bromo-2,6-difluorophenyl)methoxy)-5-((((4-(1-pyrrolidinyl)butyl)amino)carbonyl)amino)-
所屬類別
生物化工：激動劑抑制劑物理化學(xué)性質(zhì)
沸點548.6±50.0 °C(Predicted)
密度1.532
儲存條件Sealed in dry,2-8°C
溶解度DMSO: 94 mM
酸度系數(shù)(pKa)12.50±0.70(Predicted)
形態(tài)A solid
顏色White to light yellow
常見問題列表
生物活性
CP-547632 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 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 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 (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 (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 (oral; 50 mg/kg; a single oral dose) yieldes plasma concentrations above 500 ng/ml for 12 hours.
| Animal Model: | Athymic female mice (CD-1 nu/nu) bearing tumors (75-150 mm in size) |
| Dosage: | 6.25, 12.5, 25, 50, 100 mg/kg |
| Administration: | PO; daily; 10-24 days |
| Result: | Caused a dose-dependent inhibition of growth in Colo-205, DLD-1, and MDA-MB-231 xenografts. |
| Animal Model: | Female athymic mice bearing H-Ras tumor |
| 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. |