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WYE-687 CAS: 1062161-90-3

Category: Inhibitors
Product Name: WYE-687
Cat No: I000312
CAS No: 1062161-90-3
Synonyms: methyl N-[4-[4-morpholin-4-yl-1-[1-(pyridin-3-ylmethyl)piperidin-4-yl]pyrazolo[3,4-d]pyrimidin-6-yl]phenyl]carbamate
Molecular Formula: C28H32N8O3
Molecular Weight: 528.61
InChI: None
InChIKey: None
Solubility: 10 mM in DMSO
Target: mTOR
IC50: 7 nM
Storage: powder
CAS 1062161-90-3,WYE-687
  • 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 nM
Target: mTOR
WYE-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.

  • Spec

Appearance:white solid powder
Purity: > 98%

  • References

1:Concurrent inhibition of mTORC1 and mTORC2 by WYE-687 inhibits renal cell carcinoma cell growth in vitro and in vivo. Pan XD, Gu DH, Mao JH, Zhu H, Chen X, Zheng B, Shan Y.PLoS One. 2017 Mar 3;12(3):e0172555. doi: 10.1371/journal.pone.0172555. eCollection 2017. PMID: 28257457 Free PMC Article
2:Preclinical evaluation of WYE-687, a mTOR kinase inhibitor, as a potential anti-acute myeloid leukemia agent. Cheng F, Wang L, Shen Y, Xia J, Chen H, Jiang Y, Lu M.Biochem Biophys Res Commun. 2016 Feb 5;470(2):324-30. doi: 10.1016/j.bbrc.2016.01.054. Epub 2016 Jan 11. PMID: 26792718

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