AG 538是一种有效的IGF-1R竞争性抑制剂（IGF-1受体激酶，IC | 50 | = 400 nM）。对于IGF-1R底物，反应是竞争性的。还抑制了IGF-1R，IR，EGF-R和Src（IC | 50 | = 60 nM，113 nM，370 nM和2.4μM）的PTK底物聚（Glu，Tyr）的磷酸化。以更高的浓度（IC | 50 | = 76μM）抑制PKB的磷酸化。 AG 538 is a potent, competitive inhibitor of IGF-IR (IGF-1 receptor kinase, IC|50|= 400 nM). Reaction is competitive with respect to IGF-1R substrate. Also inhibits the phosphorylation of PTK substrate poly(Glu,Tyr) by IGF-1R, IR, EGF-R, and Src (IC|50|= 60 nM, 113 nM, 370 nM, and 2.4 μM, respectively). Inhibits the phosphorylation of PKB at a much higher concentration (IC|50|= 76 μM).