中文同义词:
血管生成抑制剂(E7820);化合物E7820
英文同义词:
E-7820;ER 68203-00;3-cyano-N-(3-cyano-4-methyl-1H-indol-7-yl)benzenesulfonamide;N-(3-cyano-4-methyl-1H-indol-7-yl)-3-cyanobenzene-sulfonamide;E 7820; E-7820;CS-2701;ER68203-00;E7820;E-7820;E 7820;289483-69-8;Benzenesulfonamide, 3-cyano-N-(3-cyano-4-methyl-1H-indol-7-yl)-
沸点
626.2±65.0 °C(Predicted)
密度
1.48±0.1 g/cm3(Predicted)
酸度系数(pKa)
8.17±0.30(Predicted)
生物活性
E7820是独特的血管生成抑制剂，具有抗肿瘤活性。
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 IC 50 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 IC 50 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.
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.
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.
