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AG1024 is an inhibitor of insulin-like growth factor-1 receptor (IGF-1R) and insulin receptor (IR) that specifically inhibits autophosphorylation of IGF-1R and IR with IC50 values of 7μM and 57 μm, respectively [1].

AG1024 has shown to inhibit IGF-1- and insulin-stimulated cellular proliferation in NIH-3T3 mouse fibroblast cells with IC50 values of 0.4μM and 0.1μM, respectively. Additionally, AG1024 shows to block tyrosine kinase activity towards exogenous substrates (TKA) with IC50 values of 18μM and 80μM [1].

AG1024 has been reported to block receptor tyrosine kinase activity, resulting in abolishment of MAPK and Akt pathways and inhibition of cell growth. Moreover, studies showed that AG1024 concentration-dependently inhibited E2 stimulation in MCF-7:PF cells [2].

References:

[1] Párrizas M1, Gazit A, Levitzki A, Wertheimer E, LeRoith D. Specific inhibition of insulin-like growth factor-1 and insulin receptor tyrosine kinase activity and biological function by tyrphostins. Endocrinology. 1997 Apr;138(4):1427-33.

[2] Fan P1, Agboke FA1, McDaniel RE1, Sweeney EE1, Zou X1, Creswell K1, Jordan VC2.Inhibition of c-Src blocks oestrogen-induced apoptosis and restores oestrogen-stimulated growth in long-term oestrogen-deprived breast cancer cells. Eur J Cancer. 2014 Jan; 50(2):457-68.

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