OSI-906 is a potent inhibitor of the insulin-like growth factor 1 receptor (IGF-1R) and insulin receptor (InsR), both of which play key roles in cancer cell proliferation and survival. It has been primarily investigated for its antitumor activity in various solid tumors, especially those driven by dysregulation of the IGF signaling pathway. It has shown promise in preclinical models of cancers such as lung, prostate, and sarcoma. By blocking IGF-1R and InsR phosphorylation, OSI-906 disrupts downstream signaling pathways like PI3K/AKT and MAPK, leading to cell cycle arrest and apoptosis. It was evaluated in clinical trials to assess its efficacy either as a monotherapy or in combination with other anticancer agents, particularly in patients with advanced or refractory cancers. Despite challenges related to efficacy and metabolic side effects in later-stage trials, OSI-906 remains a valuable tool compound for studying IGF-1R-driven oncogenesis.