E7820 是具有口服活性芳香族磺酰胺衍生物，是一种血管生成抑制剂，可抑制内皮上整合素 α2 亚基的表达。它调节 α1，α2，α3 和 α5 整联素 mRNA 表达，具有抗血管生成和抗肿瘤活性。它抑制大鼠主动脉血管生成，IC50为 0.11 μg/ml。

E7820 is an angiogenesis inhibitor by suppressing integrin a2 (a cell adhesion molecule expressed on endothelial cells).

E7820 inhibits proliferation of HUVEC induced by either bFGF (IC50: 0.10 μg/mL) and VEGF (IC50: 0.081 μg/mL) in serum-free medium. E7820 also inhibits both bFGF- (IC50: 0.20 μg/mL) and VEGF-driven (IC50: 0.24 μg/mL) tube formation of HUVEC in this assay[3].

E7820 (50 mg/kg) with erlotinib has a significantly synergistic antitumor effect in three xenograft models without severe body weight loss. E7820 (50 mg/kg) and erlotinib decrease MVD and enhance apoptosis in tumor-associated endothelial cells, inhibit tumor cell proliferation and enhanced apoptosis, and enhance inhibition of cell proliferation and apoptosis through activation of both intrinsic and extrinsic apoptosis pathways in human NSCLC xenograft models[1]. E7820 shows anti-tumor activity at doses of 50, 100, and 200 mg/kg in the tumor growth and α2-integrin expression experiments[2]. E7820 (50, 100, and 200 mg/kg) inhibits tumor growth in a dose-dependent manner in all s.c. xenograft models. E7820 completely inhibits s.c. tumor growth of LoVo tumor cells and also regresses the tumor mass of KP-1 tumor cells at the dosages of both 100 and 200 mg/kg[3].

289483-69-8

C17H12N4O2S

336.37

ER68203-00

H2O:Insoluble
DMSO:33 mg/mL
Powder: -20°C for 3 years
In solvent: -80°C for 2 years