AG-1024

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AG-1024 is a selective IGF-1R inhibitor with an IC50 of 0.4 μM. Exposure to Tyrphostin AG 1024 inhibits proliferation of cell and triggers their apoptosis in a time-dependent manner. Tyrphostin AG 1024 prevents the growth inhibition for IC20 plus irradiation (4 Gy) by 50% compared to the control.Examination of Tyrphostin AG 1024 effects on radiation response demonstrates a marked enhancement in radiosensitivity and amplification of radiation-induced apoptosis. Tyrphostin AG 1024-induced apoptosis is associated with a downregulation of expression of phospho-Akt1, increased expression of Bax, p53 and p21, and a decreased expression of bcl-2 expression, especially when combined with irradiation. Tyrphostin AG 1024 is an effective anti-proliferative agent for breast carcinoma cells MCF-7. IGF1-R inhibitor tyrphostin AG1024 (10 μm) restores H358 cells apoptosis when cultured in serum-free medium. Incubation with AG1024 markedly decreases the AR level detected in the serum-free culture medium. AG1024 reduces IGF1 release in the serum-free culture medium. AG1024 enhances the apoptosis-inducing effect of gefitinib.Tyrphostin AG1024 significantly inhibits signal transmission by Akt (PKB), ERK (1/2), Src and STAT.The cytotoxic effect of AG1024 is more than 100 times greater on nutrient-deprived PANC-1 cells (NDM) with an IC50 of 55 nM, relative to cells in nutrient-sufficient medium (DMEM) with an IC50 of 21 μM. In DMEM, 0.3 μM AG1024 does not induce any significant PANC-1 cell death as determined using propidium iodide and annexin V staining and flow cytometry. In contrast, 34% of the cells grown in NDM and treated with the same concentration of AG1024 reveals propidium iodide-positive/annexin V-negative staining. In addition, AG1024 gives rise to significant increases in neuronal ADDL binding both when AG1024 is added alone and in the presence of exogenous insulin.

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