产品
编 号:F307254
分子式:C17H12N4O2S
分子量:336.37
产品类型
结构图
CAS No: 289483-69-8
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产品详情
生物活性:
E7820 (ER68203-00), an orally active aromatic sulfonamide derivative, is a unique angiogenesis inhibitor suppressing an expression of integrin alpha2 subunit on endothelium. E7820 inhibits rat aorta angiogenesis with an IC50 of 0.11 μg/ml. E7820 modulates α-1, α-2, α-3, and α-5 integrin mRNA expression. Antiangiogenic and antitumor activity.
体内研究:
E7820 (ER68203-00) (50-200 mg/kg; p.o. ; twice daily for 14 days) delays the growth of WiDr cells inoculated s.c..E7820 (200-400 mg/kg; p.o.;once daily for 4 days) potently inhibits WiDr-induced angiogenesis.Animal Model:Six-week-old female nude mice (KSN mice, WiDr-induced angiogenesis model)
Dosage:50, 100, 200 mg/kg
Administration:p.o. ;twice daily for 14 days from 2 days after inoculation of the tumor cells
Result:The antitumor effect was dose-dependent at 50, 100, and 200 mg/kg, and the tumor growth rates were 52%, 46%, and 27%, respectively.
体外研究:
E7820 (ER68203-00) inhibits both bFGF- and VEGF-driven ube formation of human umbilical vascular endothelial cell (HUVEC) in a dose-dependent manner with IC50 of 0.20 and 0.24 μg/ml, respectively.?E7820 inhibits proliferation of HUVEC induced by either bFGF or VEGF in serum-free medium (SFM). The IC50 values are 0.10 and 0.081 μg/ml, respectively. Antiproliferative activity of E7820 against both WiDr and LoVo cells is very weak compared with that against HUVEC. The values of IC50 were 29 and 15 μg/ml, respectively.