Description | An IGF-1R inhibitor (IC50 = 0.15 µM in a cell-free assay); selective for IGF-1R over a panel of 20 kinases but also inhibits InsR, FLT1, FLT3, and Tie2 (IC50s = 0.14, 0.6, 0.42, and 0.53 µM, respectively, in cell-free assays); selectively inhibits the autophosphorylation of IGF-1R over InsR, EGFR, PDGFR, c-Kit, and Bcr-Abl in cells (IC50s = 0.086, 2.3, >10, >10, >5, and >10 µM, respectively); reduces tumor volume in an NWT-21 murine fibrosarcoma model at 20, 30, or 50 mg/kg twice per day |