IGF-1R (insulin-like growth factor-1 receptor) plays a key role in transformation, growth and survival of malignant cells, and has been considered as a general and promising target for cancer treatment. AG1024 is a selective IGF-1R inhibitor with IC50 value of 7μM for inhibition of IGF-1R autophosphorylation in NIH-3T3 cells, also inhibits IR with IC50 of 57μM. AG1024 inhibited the IGF-1-induced MAPK signal-regulated kinase pathway in metastatic melanoma cells (501 mel) treated with 4μM AG1024 for 30min. And a longer treatment of AG1024 led to a restore of pRb tumor suppressive function as the reduction in the phosphorylated forms of pRb, p107 and p130 due to proteasomal and nonproteasomal degradation, and the formation of growth suppressive DNA binding complexes consisting of pRb and E2F1 or E2F3 could be observed[2].
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