AZD-5363isanoralpan-AKTinhibitorthatcauseshyperphosphorylationofAKT,lockingitinacatalyticallyinactivestate,unabletophosphorylatedownstreamsignalingsubstratessuchasPRAS40andGSK-β.Thiscompounddisplaysanticancerchemotherapeuticactivity,inhibitingproliferationandinducingtumorregressionininvitroandinvivomodelsofHER2+breastcancerandprostatecancer.AZD-5363mayalsoexhibitinhibitoryactivityagainstRho-associatedproteinkinase(ROCK),p70S6K,PKA,MKK1,MSK1,MSK2,PKC,PKG,PRKX,andRSK2/3.
| CasNo. | 1143532-39-1 |
|---|---|
| Purity | ≥99%,≥99%ee |
| Formula | C21H25ClN6O2 |
| FormulaWt. | 428.92 |
| IUPACName | 4-amino-N-[(1S)-1-(4-chlorophenyl)-3-hydroxypropyl]-1-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)piperidine-4-carboxamide |
| Synonym | AZD5363 |
| Solubility | InDMSO,waterwith2eq.ofacid |
| Appearance | WhiteCrystalPowder |
| StoreTemp | -20°C |
|---|---|
| ShipTemp | Ambient |
| MSDS | A9601MSDSPDF |
|---|---|
| InfoSheet | A9601InfoSheetPDF |
| Brochures | PI3K-Akt-mTORCPathwayBooklet |
AddieM,BallardP,ButtarD,etal.Discoveryof4-amino-N-[(1S)-1-(4-chlorophenyl)-3-hydroxypropyl]-1-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)piperidine-4-carboxamide(AZD5363),anorallybioavailable,potentinhibitorofAktkinases.JMedChem.2013Mar14;56(5):2059-73.PMID:23394218.
LamoureuxF,ThomasC,CrafterC,etal.BlockedautophagyusinglysosomotropicagentssensitizesresistantprostatetumorcellstothenovelAktinhibitorAZD5363.ClinCancerRes.2013Feb15;19(4):833-44.PMID:23258740.
DaviesBR,GreenwoodH,DudleyP,etal.PreclinicalpharmacologyofAZD5363,aninhibitorofAKT:pharmacodynamics,antitumoractivity,andcorrelationofmonotherapyactivitywithgeneticbackground.MolCancerTher.2012Apr;11(4):873-87.PMID:22294718.
