Orally active insulin-like growth factor 1 receptor (IGF1R) inhibitor that exhibits no activity at the insulin receptor, FGFR, PDGFR or EGFR. Inhibits IGF1R autophosphorylation (IC50 ~ 1 nM), increases the fraction of cells in the G2/M phase and upregulates apoptosis. Exhibits antiproliferative effects in multiple cancer cell lines (IC50 = 0.05 - 15 μM), and has anticancer and antineovascularization activity in vivo.