| Identification | Back Directory | [Name]
WYE-354 | [CAS]
1062169-56-5 | [Synonyms]
CS-441
WYE-354
WYE-354 USP/EP/BP
WYE-354 (Degrasyn)
WYE-354;WYE 354; WYE354
Methyl 4-(6-(4-(methoxycarbonylamino)phenyl)-4-morpholino-1H-pyrazolo[3,4-d]pyrimidin-1-yl)pip
methyl 4-[6-[4-(methoxycarbonylamino)phenyl]-4-morpholin-4-ylpyrazolo[3,4-d]pyrimidin-1-yl]piperidine-1-carboxylate
4-[6-[4-[(Methoxycarbonyl)amino]phenyl]-4-(4-morpholinyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl]-1-piperidinecarboxylic acid methyl ester
1-Piperidinecarboxylic acid, 4-[6-[4-[(methoxycarbonyl)amino]phenyl]-4-(4-morpholinyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl]-, methyl ester | [Molecular Formula]
C24H29N7O5 | [MDL Number]
MFCD18074514 | [MOL File]
1062169-56-5.mol | [Molecular Weight]
495.53 |
| Chemical Properties | Back Directory | [density ]
1.46 | [storage temp. ]
Sealed in dry,Store in freezer, under -20°C | [solubility ]
≥49.6 mg/mL in DMSO; insoluble in H2O; insoluble in EtOH | [form ]
solid | [pka]
13.42±0.70(Predicted) |
| Hazard Information | Back Directory | [Description]
WYE-354 is a potent cell-permeable inhibitor of mTOR (IC50 = 4.3 nM) which blocks signaling through both mTOR complex 1 (mTORC1) and mTORC2.1,2 It is a much weaker inhibitor of phosphatidylinositol 3-kinase α (IC50 = 1,026 nM) and other kinases.3 WYE-354 induces G1 cell cycle arrest in both rapamycin-sensitive and rapamycin-resistant cancer cell lines, inhibits mTORC1 and mTORC2 in tumor-bearing mice, and reduces tumor growth in nude mice with PTEN-null tumors.1 | [Uses]
A 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. | [Definition]
ChEBI: 4-[6-[4-(methoxycarbonylamino)phenyl]-4-(4-morpholinyl)-1-pyrazolo[3,4-d]pyrimidinyl]-1-piperidinecarboxylic acid methyl ester is a carbamate ester. | [target]
mTOR | [References]
[1] qingsong liu, carson thoreen, jinhua wang, david sabatini, nathanael s. gray. mtor mediated anti-cancer drug discovery. drug discovery today. 2009. 6(2): 47-55.
[2] shi-yong sun. mtor kinase inhibitors as potential cancer therapeutic drugs. cancer letters. 28 october 2013. 340(1): 1-8. |
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