WYE 354-d3

Catalogue number C262546
Chemical nameWYE 354-d3
CAS Number1794791-66-4
Synonyms4-[6-[4-[[(Methoxy-d3)carbonyl]amino]phenyl]-4-(4-morpholinyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl]-1-piperidinecarboxylic Acid Methyl Ester; WYE-354-d3;
Molecular WeightC24H26D3N7O5
Physical DescriptionPowder
SolventChloroform, Dichloromethane,DMSO
StorageStored at 2-8°C, Protected from air and light, refrigerate or freeze
ApplicationsA labelled pyrazolopyrimidines derivative that is a potent and ATP-competitive mTOR inhibitor with much reduced activity against PI 3-Kα or PI 3-Kγ. WYE-354 is equally potent against mTORC1 and mTORC2 activities in HEK293 immune complex kinase assays using S6K and Akt as the respective substrate (IC50 <200 nM; [ATP] = 100 µM) and effectively blocks cellular phosphorylation of S6K on T389 and Akt on S473 both in cultures and in a murine xenograft model, resulting in a significant suppression of PC3MM2-derived tumor growth (by 86% on day 7; 50 mg/kg, i.p twice per day) in vivo.
ReferencesYu, K. et al.: Cancer Res., 69, 6232 (2009); Zask, A. et al.: J. Med. Chem., 52, 5-13 (2009); Dormind-Meuwly, A. et al.: Biochem. Biophys. Res. Comm., 407, 714 (2011);
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10mg$1600.0010% OFF
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