"目录号: HY-15271
PI3K/Akt/mTOR-
WYE-687是ATP竞争性mTOR选择性抑制剂，比对PI3Kα/γ的抑制性高超过100倍。
mTOR
相关产品
Rapamycin-Everolimus-AP1903-INK-128-BEZ235-Torin 1-AP20187-AZD-8055-MHY1485-PP 242-LY3023414-AZD2014-PF-04691502-Temsirolimus-Torin 2-
生物活性
Description
WYE-687 is an ATP-competitive and selective inhibitor of mTOR with IC50 of 7 nM; > 100 fold selectivity for mTOR than PI3Kα/γ.IC50 value: 7 nMTarget: mTORWYE-687 is a potent ATP-competitive mTOR inhibitor with an IC50 of 7 nM. It is well reported that the mammalian target of rapamycin (mTOR) is centrally involved in cell growth, metabolism, and angiogenesis. Significantly, the pyrazolopyrimidines were selective for mTOR over PI3Kα (>100-fold) and PI3Kγ (>500-fold) and were poorly active in a panel of 24 protein kinases. Unlike the rapalogs, WYE-687 acutely blocked mTORC2-dependent phosphorylation of AKT in vitro and in vivo. In various cancer cells, WYE-687 inhibited the mTORC1 substrate P-S6K(T389) and mTORC2 substrate P-AKT(S473) at submicromolar concentrations without significant inhibition of P-AKT(T308). WYE-687 was identified as an ATP-competitive, and selective inhibitor of mTOR kinase activity.
References
[1].Yu K, Toral-Barza L, Shi C, Zhang WG, Lucas J, Shor B, Kim J, Verheijen J, Curran K, Malwitz DJ, Cole DC, Ellingboe J, Ayral-Kaloustian S, Mansour TS, Gibbons JJ, et al. Biochemical, cellular, and in vivo activity of novel ATP-competitive and selective