E7820

"目录号: HY-14571

Cytoskeleton-

E7820 是一种血管生成抑制剂，能够抑制整合素蛋白 a2 (integrin a2) 的活性，整合素蛋白 a2 是内皮细胞中的细胞粘附分子。

Integrin

生物活性

Description

E7820 is an angiogenesis inhibitor by suppressingintegrin a2, a cell adhesion molecule expressed on endothelial cells.

In Vitro

E7820 treatment inhibits proliferation of HUVEC induced by either bFGF and VEGF in serum-free medium with IC50values of 0.10 and 0.081 μg/mL, respectively. E7820 also inhibits both bFGF- and VEGF-driven tube formation of HUVEC in this assay. The IC50values are 0.20 and 0.24 μg/mL, respectively[3].

In Vivo

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].

Clinical Trial

NCT00309179

Eisai Inc.

Advanced Colorectal Cancer

September 2007

Phase 2

NCT01773421

Eisai Inc.

Advanced Solid Tumors

July 8, 2011

Phase 1

NCT00078637