Cat. No. Name Size Price Add Cart
KI0542WYE-3545 mg$192
WYE-35410 mg$220
WYE-35450 mg$880

Chemical Characteristic

Product NameWYE-354
CAS No.1062169-56-5
Molecular Weight 495.53
FormulaC24H29N7O5
Chemical Name4-[6-[4-[(Methoxycarbonyl)amino]phenyl]-4-(4-morpholinyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl]-1-piperidinecarboxylic acid methyl ester
SmilesN1(CCC(CC1)n1c2nc(nc(c2cn1)N1CCOCC1)c1ccc(cc1)NC(=O)OC)C(=O)OC
Chemical Structure

Biological activities

WYE-354 is a potent and ATP-competitive inhibitor of mTOR. The IC50 value of WYE-354 against mTOR is 5 nM. WYE-354 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-354 also induces a small but significant amount of PARP cleavage in the PTEN-null LNCap cells but not in HCT116 or HT29 cells. WYE-354 shows antiproliferative effects in MDA361 and U87MG cells involving G1 cell cycle arrest and selective induction of apoptosis. WYE-354 down-regulates angiogenic factors.[1] In vitro, WYE-354 also induces phosphorylation and inactivation of the translation elongation factor eEF2 in MDA361 cells.[2] When injected into tumor-bearing mice, WYE-354 inhibits mTORC1 and mTORC2 and displays robust antitumor activity in PTEN-null tumors. In vivo, WYE-354 treatment (50 mg/kg ) achieves dose-dependent suppression of tumor growth.[1]

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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