AG-1024 (C09-0734-772)

InformationAG-1024 AG-1024 (Tyrphostin, AGS 200) inhibits IGF-1R autophosphorylation with IC50 of 7 μM, is less potent to IR with IC50 of 57 μM and specifically distinguishes between InsR and IGF-1R (as compared to other tyrphostins).In vitroAG-1024 blocks the IGF-1 receptor and IR autophosphorylation with IC50 of 7 μM and 57 μM, respectively. AG-1024 also inhibits the receptor tyrosine kinase activity towards exogenous substrates (TKA) with IC50 values of 18 μM and 80 μM, respectively. AG-1024 (10 μM) inhibits cell proliferation in a time-dependent manner, and induces apoptosis in MCF-7 cells at 48 hours by 20.1% and >40% when combined with irradiation (10 Gy), more potently than that of irradiation (10 Gy) alone by 11.8%, which is associated with a down-regulation of phospho-Akt1 and bcl-2, and up-regulation of Bax, p53 and p21. AG-1024 significantly inhibits melanoma cell proliferation with an IC50 of <50 nM in the absence of serum, by blocking MAPK/ERK2 signaling, subsequently rapidly inducing pRb dephosphorylation and activation, and eventually the formation of growth suppressive pRb-E2F complexes. AG-1024 treatment down-regulates the expression of Bcr-Abl and P-Akt, and up-regulates DNA-PKcs expression in UT7-9 and Ba/F3-p210 cells, leading to decreased clonogenic survival and proliferation. AG-1024 also significantly inhibits the proliferation of cells resistant to the BCR-ABL inhibitor STI571, which correlates with a dose-dependent decrease in Bcr-Abl protein expression.In vivoAdministration of AG-1024 at a dose of 30 μg for 10 days significantly inhibits the tumor growth of Ba/F3-p210 xenograft in mice.Cell Datacell lines：Concentrations：Dissolved in DMSO, final concentration 10 μMIncubation Time：24, 48 or 72 hoursPowder Purity:≥99%. Specification: 10mM in DMSO Molecular Formula: C14H13BrN2O Molecular Weight: 305.17