AG-1024 (Tyrphostin) |cas 65678-07-1| DC Chem|Supplier|Price|Buy
AG-1024 (Tyrphostin) |cas 65678-07-1| DC Chem|Supplier|Price|Buy
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AG-1024 (Tyrphostin) |cas 65678-07-1 ,Synonym: AG-1024; Tyrphostin AG 1024 ,Chemical name: 2-(3-bromo-5-tert-butyl-4-hydroxybenzylidene)malononitrile ,Molecular Formula: C14H13BrN2O ,MW:305.17
AG-1024 (Tyrphostin) , cas 65678-07-1,Purity: >98%, Best Price and quality from DC Chemicals. AG-1024 (Tyrphostin) inhibits IGF-1R autophosphorylation with IC50 of 7 μM, less potent to IR with IC50 of 57 μM.
AG-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. [1] 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. [2] 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. [3] 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. [4] Administration of AG-1024 at a dose of 30 μg for 10 days significantly inhibits the tumor growth of Ba/F3-p210 xenograft in mice. [4]
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