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

生物活性靶点体外研究体内研究 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-甲酰胺试剂级价格

CAS号:252003-65-9
英文名:CP-547632
中文名: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
CBNumber:CB82473822
分子式:C20H24BrF2N5O3S
分子量:532.4
MOL File:252003-65-9.mol

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-甲酰胺化学性质

沸点 :548.6±50.0 °C(Predicted)
密度 :1.532
储存条件 :2-8°C
溶解度 :DMSO: 94 mM
形态 :A solid
酸度系数(pKa) :12.50±0.70(Predicted)
颜色 :White to light yellow

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、用途与生产工艺

生物活性 CP-547632 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 对 VEGFR2 和 bFGF 的选择性高于 EGFR，PDGFRβ 和相关的酪氨酸激酶 (TKs)。CP-547632 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 (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 (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.