FGFR1/VEGFR2-IN-2

Description

FGFR1/VEGFR2-IN-2 compound 6l is a VEGFR2/FGFR1 dual inhibitor. The IC50 values for VEGFR2 and FGFR1 are 0.025 AAasAasAAmuM and 0.026 AAasAasAAmuM respectively, and for EGFR and PDGFR-?, the IC50 values are 0.106 AAasAasAAmuM and 0.077 AAasAasAAmuM. FGFR1/VEGFR2-IN-2 showes significant anti-cancer activity GI=60.38 % on NCI-60 cell line, with an IC50 of 8.51 AAasAasAAmuM in T-47D cell line and anti-migration. FGFR1/VEGFR2-IN-2 acts to arrest cells in the G1 phase and promote apoptosis and necrosis; the IC50 for MCF-7 cell line exceeds 100 AAasAasAAmuM, and the IC50 for MDA-MB-231 is 69.17 AAasAasAAmuM, non-toxic to normal cells.