产品描述:
AST-1306 is an irreversible inhibitor of EGFR, HER2, and HER4 (IC50s = 0.5, 3, and 0.8 nM, respectively).{48897} It is selective for EGFR, HER2, and HER4 over a panel of 23 additional kinases (IC50s = >10 µM). AST-1306 also inhibits EGFRT790M/L858R with an IC50 value of 12 nM in a cell-free assay. It decreases EGFR, ERK1/2, and Akt phosphorylation in Calu-3, A549, and SKOV3 cancer cells when used at concentrations ranging from 0.001 to 1 µM. AST-1306 inhibits proliferation of Calu-3, BT474, MDA-MB-468, A549, SKOV3, NCI H23, and MCF-7 cells (IC50s = 0.23-16 µM). It reduces tumor growth in Calu-3, A549, SKOV3, and HO8910 mouse xenograft models when administered at doses of 25, 50, and 100 mg/kg per day.