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). 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 alpha2 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.Formal Name: 3-cyano-N-(3-cyano-4-methyl-1H-indol-7-yl)-benzenesulfonamide. CAS Number: 289483-69-8. Molecular Formula: C17H12N4O2S. Formula Weight: 336.4. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 30 mg/ml, DMF:PBS (pH 7.2) (1:4): 0.20 mg/ml, DMSO: 20 mg/ml. lambdamax: 219, 284 nm. SMILES: O=S(C1=CC(C#N)=CC=C1)(NC2=CC=C(C)C3=C2NC=C3C#N)=O. InChi Code: InChI=1S/C17H12N4O2S/c1-11-5-6-15(17-16(11)13(9-19)10-20-17)21-24(22,23)14-4-2-3-12(7-14)8-18/h2-7,10,20-21H,1H3. InChi Key: LWGUASZLXHYWIV-UHFFFAOYSA-N.