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Palomid 529 (P529) is a novel potent antitumour PI3K/Akt/mTOR inhibitor with a GI50 of <35 μM in the NCI-60 cell lines panel.[1] Palomid 529 inhibits both VEGF-driven and bFGF-driven endothelial cell proliferation with IC50 of 20 nM and 30 nM, respectively.

PI3K activates AKT,then AKT activate CREB,inhibit p27locate FOXO in the cytoplasm, activate PtdIns-3ps, and mTOR which can effect transcription of p70 or 4EBP1.[2,3]

In many cancers, this pathway is overactive, thus reducing apoptosis and allowing proliferation. This pathway is necessary, however, to promote growth and proliferation over differentiation of adult stem cells, neural stem cells specifically. Additionally, this pathway has been found to a be a necessary component in neural long term potentiation.[4]Lowering the effect of the PI3K pathway and increasing the effect of GSK3β and HB9 in NSCs is a potential way of generating these cells better for survival of the neurons. Amplifying the PI3K/AKT pathway increases this neural outgrowth which can determine appropriate treatment concentrations of bisperoxovanadium to stimulate axonal outgrowth but not cause cancer.Not only Palomid 529 inhibits radiation-induced overexpression of Id-1 and VEGF, but also down-regulates radiation-induced MMP-2 and MMP-9. [5]

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