Linsitinib (OSI-906) is a potent inhibitor of IGF-1R (35 nM), Insulin Receptor (75 nM), ABCG2 (1000, 2000 nM), ABCC10 (1000, 2000 nM), TSHR, AKT, ERK1/2, S6K, S6, 4EBP1, GSK3B, and AMPK. Linsitinib (OSI-906) exhibits the greatest inhibitory potency toward IGF-1R (IC50 = 35 nM).