AG-1024 is a selective IGF-1R kinase inhibitor with modest activity. It inhibits insulin-stimulated cellular proliferation with IC50 of 0.4 µM. [1] AG-1024 showed synergistic effect with irradation and inhibited proliferation and induced apoptosis in human breast cancer MCF-7 cells. [2] AG-1024 also inhibited autocrine growth of human prostate cancer DU145 cells with an IC50 value of 2.5 µM.[3]

In vivo, daily administration of AG-1024 through i.v. route at 1-2 mg/kg has been shown to increase the survival rate of mouse injected with Ba/F3-p210 cells. [4]