Cat. No. Name Size Price Add Cart
KI0545WYE-6875 mg$374
WYE-68710 mg$592
WYE-68750 mg$1620
WYE-687200 mg$3000

Chemical Characteristic

Product NameWYE-687
CAS No.1062161-90-3
Molecular Weight 528.61
FormulaC28H32N8O3
Chemical NameN-[4-[4-(4-Morpholinyl)-1-[1-(3-pyridinylmethyl)-4-piperidinyl]-1H-pyrazolo[3,4-d]pyrimidin-6-yl]phenyl]carbamic acid methyl ester
SmilesC(=O)(Nc1ccc(cc1)c1nc2c(c(n1)N1CCOCC1)cnn2C1CCN(CC1)Cc1cnccc1)OC
Chemical Structure

Biological activities

WYE-687 is a potent and ATP-competitive inhibitor of mTOR. The IC50 value of WYE-687 against mTOR is 7 nM. WYE-687 dose dependently inhibits mTORC2-specific substrate His6-AKT or the mTORC1 substrate His6-S6K. WYE-687 profoundly inhibits cap-dependent and global protein synthesis in human breast cancer cell line MDA361. WYE-687 also shows antiproliferative effects in MDA361 and U87MG cells involving G1 cell cycle arrest and selective induction of apoptosis. WYE-687 down-regulates angiogenic factors.[1] In vitro, WYE-687 also induces phosphorylation and inactivation of the translation elongation factor eEF2 in MDA361 cells.[2]

References

[1] Yu K, et al. Biochemical, cellular, and in vivo activity of novel ATP-competitive and selective inhibitors of the mammalian target of rapamycin. Cancer Res. 2009, 69(15): 6232-6240.
[2] Shor B, et al. Targeting mTOR globally in cancer: thinking beyond rapamycin. Cell Cycle. 2009, 8(23): 3831-3837.

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