Potent and selective insulin-like growth factor-1 receptor (IGF-IR) and insulin receptor (IR) kinase inhibitor with additional affinity for anaplastic lymphoma kinase (ALK) with IC50 values of 2.0 nM, 1.6 nM, and 0.6 nM, for IGF1R, IR, and ALK respectively, and >800-fold selectivity over related kinases, including RSK1, JNK3, and B-Raf V600EGSK 1838705A inhibits the proliferation of cancer cell lines, comprises the growth of human tumor xenografts in vivo, and causes complete regression of ALK-dependent tumors in vivo at well-tolerated doses.