E7820

E7820 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).¹ 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.²

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1. Funahashi, Y., Sugi, N.H., Semba, T., et al. Sulfonamide derivative, E7820, is a unique angiogenesis inhibitor suppressing an expression of integrin α2 subunit on endothelium. Cancer Res. 62(21), 6116-6123 (2002).

2. Semba, T., Funahashi, Y., Ono, N., et al. An angiogenesis inhibitor E7820 shows broad-spectrum tumor growth inhibition in a xenograft model: Possible value of integrin α2 on platelets as a biological marker. Clin. Cancer Res. 10(4), 1430-1438 (2004).