Linsitinib（OSI-906）是一种高效、选择性和口服可用的IGF-1受体和胰岛素受体（IR）的双重抑制剂，IC50分别为35 nM和75 nM。

NVP-AEW541 (AEW541) 是一种口服活性的胰岛素样生长因子 1 受体 (IGF-1R) 抑制剂，IC50 为 0.15 μM。它还抑制胰岛素受体 (InsR)，IC50 为 0.14 μM，显示出显著的抗肿瘤活性。

BMS-536924 is an ATP-competitive IGF-1R/IR inhibitor with IC50 of 100 nM/73 nM.

AG1024 inhibits IGF-1R autophosphorylation with IC50 of 7 μM, less potent to IR with IC50 of 57 μM.

BMS-754807 is a potent and reversible inhibitor of IGF-1R/InsR with IC50 of 1.8 nM/1.7 nM, less potent to Met, Aurora A/B, TrkA/B and Ron, and shows little activity to Flt3, Lck, MK2, PKA, PKC etc.

GSK1904529A is a selective inhibitor of IGF-1R and IR with IC50 of 27 nM and 25 nM, being > 100-fold selective for IGF-1R/InsR than Akt1/2, Aurora A/B,B-Raf, CDK2, EGFR etc.

GSK1838705A is a potent small-molecule IGF-IR, the insulin receptor and anaplastic lymphoma kinase (ALK) inhibitor with IC50 of 2.0, 1.6 and 0.5 nM, respectively.