E 7820

DescriptionE7820 is a sulfonamide derivative and an angiogenesis inhibitor that inhibits bFGF- and VEGF-stimulated human umbilical vein endothelial cell (HUVEC) proliferation (IC50s = 0.1 and 0.081 μg/ml, respectively). It inhibits bFGF- and VEGF-stimulated tube formation of HUVECs in a concentration-dependent manner (IC50s = 0.2 and 0.24 μg/ml, respectively). E7820 selectively decreases the surface expression and mRNA levels of integrin α2 over CD31 and VE-cadherin in HUVECs. In vivo, E7820 (200 and 400 mg/kg) reduces tumor growth and inhibits angiogenesis in a WiDr colorectal cancer mouse xenograft model. It also reduces tumor weight in a panel of seven human colon, breast, pancreas, and kidney cancer mouse xenograft models, completely inhibits tumor growth in KP-1 pancreatic and LoVo colon cancer mouse xenograft models, and inhibits tumor growth in KP-1 and COLO 320DM mouse orthotopic transplantation models.

UsesE7820 (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[1][2].