A dual InsR and IGF-1R kinase inhibitor (IC50s = 25 and 27 nM, respectively, in a cell-free assay); selectively inhibits InsR and IGF-1R kinases over a panel of 45 serine/threonine and tyrosine kinases (IC50s = >1 µM for all); decreases proliferation of 13 cancer cell lines including multiple myeloma, sarcoma, colon, and breast cancer cells (IC50s = 35-189 nM) in a panel of 35 cell lines; reduces tumor growth in NIH3T3-LISN, COLO 205, HT-29, and BxPC3 mouse xenograft models at 30 mg/kg for 21 days