AGL 2263 is an inhibitor of the insulin-like growth factor 1 receptor (IGF-1R; IC50 = 0.43 μM).1 It also inhibits the insulin receptor (IR), protein kinase B (PKB), and Src in a cell-free assay (IC50s = 0.4, 55, and 2.2 μM, respectively). AGL 2263 inhibits IGF-1R autophosphorylation and phosphorylation of the downstream elements IRS-1, PKB, and ERK2 in an ATP-independent manner. It inhibits colony formation of PC3 and LNCaP prostate and MCF-7 and MDA-MB-468 breast cancer cells in soft agar (IC50s = 4.3, 9, 17, and 6 μM, respectively).
1.Blum, G., Gazit, A., and Levitzki, A.Development of new insulin-like growth factor-1 receptor kinase inhibitors using catechol mimicsJ. Biol. Chem.278(42)40442-40454(2003)