3-[(4-溴-2,6-二氟苄基)氧基]-5-[3-[4-(吡咯烷-1-基)丁基]脲基]异噻唑-4-甲酰胺
中文名称 | 3-[(4-溴-2,6-二氟苄基)氧基]-5-[3-[4-(吡咯烷-1-基)丁基]脲基]异噻唑-4-甲酰胺 |
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中文同义词 | 3-[(4-溴-2,6-二氟苄基)氧基]-5-[3-[4-(吡咯烷-1-基)丁基]脲基]异噻唑-4-甲酰胺;化合物 T10870L |
英文名称 | CP-547632 |
英文同义词 | CP-547632;3-(4-Bromo-2,6-difluorobenzyloxy)-5-(3-(4-pyrrolidin-1-ylbutyl)ureido)isothiazole-4-carboxylic acid amide;4-Isothiazolecarboxamide, 3-((4-bromo-2,6-difluorophenyl)methoxy)-5-((((4-(1-pyrrolidinyl)butyl)amino)carbonyl)amino)-;CP-547632(CP 547632);3-[(4-broMo-2,6-difluorophenyl)Methoxy]-5-[[[[4-(1-pyrrolidinyl)butyl]aMino]carbonyl]aMino]-4-isothiazolecarboxaMide;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-carbox;3-[(4-Bromo-2,6-difluorobenzyl)oxy]-5-[3-[4-(pyrrolidin-1-yl)butyl]ureido]isothiazole-4-carboxamide |
CAS号 | 252003-65-9 |
分子式 | C20H24BrF2N5O3S |
分子量 | 532.4 |
EINECS号 | 200-258-5 |
相关类别 | |
Mol文件 | 252003-65-9.mol |
结构式 |
3-[(4-溴-2,6-二氟苄基)氧基]-5-[3-[4-(吡咯烷-1-基)丁基]脲基]异噻唑-4-甲酰胺 性质
沸点 | 548.6±50.0 °C(Predicted) |
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密度 | 1.532 |
储存条件 | 2-8°C |
溶解度 | 二甲基亚砜:94mM |
形态 | 固体 |
酸度系数(pKa) | 12.50±0.70(Predicted) |
VEGFR-2 11 nM (IC 50 ) |
FGFR 9 nM (IC 50 ) |
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. |
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. |
安全信息
更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
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2024/04/30 | HY-13302 | CP-547632 | 1 mg | 431元 | |
2024/04/30 | HY-13302 | 3-[(4-溴-2,6-二氟苄基)氧基]-5-[3-[4-(吡咯烷-1-基)丁基]脲基]异噻唑-4-甲酰胺 CP-547632 | 252003-65-9 | 5mg | 850元 |