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289483-69-8

中文名稱 CS-2701
英文名稱 E-7820
CAS 289483-69-8
分子式 C17H12N4O2S
分子量 336.37
MOL 文件 289483-69-8.mol
更新日期 2024/12/10 17:13:37
289483-69-8 結構式 289483-69-8 結構式

基本信息

中文別名
化合物E7820
血管生成抑制劑(E7820)
英文別名
E-7820
CS-2701
ER 68203-00
E 7820
E-7820
ER68203-00
E7820
E-7820
E 7820
289483-69-8
3-cyano-N-(3-cyano-4-methyl-1H-indol-7-yl)benzenesulfonamide
N-(3-cyano-4-methyl-1H-indol-7-yl)-3-cyanobenzene-sulfonamide
Benzenesulfonamide, 3-cyano-N-(3-cyano-4-methyl-1H-indol-7-yl)-
所屬類別
生物化工:激動劑抑制劑

物理化學性質

沸點626.2±65.0 °C(Predicted)
密度1.48±0.1 g/cm3(Predicted)
儲存條件-20°C儲存
溶解度DMSO:67.0(Max Conc. mg/mL);199.19(Max Conc. mM)
酸度系數(pKa)8.17±0.30(Predicted)
形態(tài)結晶固體
顏色Light yellow to light brown

安全數據

危險性符號(GHS)GHS hazard pictograms
GHS07
警示詞警告
危險性描述H302-H315-H319-H335

常見問題列表

生物活性
E7820是獨特的血管生成抑制劑,具有抗腫瘤活性。
體外研究

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.

體內研究

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.
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