Linsitinib (formerly OSI-906; OSI 906) is a firs-in-class, ATP-competitive and orally bioavailable dual inhibitor of and insulin receptor (IR) and insulin-like growth factor-1 receptor (IGF-1R) with potential antitumor activity. It exhibits modest potency against InsR with an IC50 of 75 nM, and it has no activity against other kinases like Abl, ALK, BTK, EGFR, FGFR1/2, PKA, and so on. In cell-free assays, it inhibits IGF-1R with an IC50 of 35 nM.
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