MK-2206isanallostericinhibitorofAktthatpreventstranslocationofAkttomembranes.MK-2206exhibitsanticancerchemotherapeuticactivityinavarietyofinvitrocancermodels;thiscompoundinducesG1-phasecellcyclearrestinhepatocellularcarcinomacells,inhibitscellproliferationinnon-smallcelllungcancercells,andinhibitsproliferationinmedullarythyroidcancercells.Inanimalmodelsofnasopharyngealcancer,MK-2006inhibitstumorgrowth.
| CasNo. | 1032349-77-1 |
|---|---|
| Purity | ≥99% |
| Formula | C25H22ClN5O |
| FormulaWt. | 443.93 |
| IUPACName | 8-[4-(1-aminocyclobutyl)phenyl]-9-phenyl-2H-[1,2,4]triazolo[3,4-f][1,6]naphthyridin-3-one;hydrochloride |
| Synonym | MK-2206hydrochloride |
| Solubility | SolubleinDMSO,waterwith1eq.ofacid |
| Appearance | off-whitepowder |
| StoreTemp | -20°C |
|---|---|
| ShipTemp | Ambient |
| MSDS | M4000MSDSPDF |
|---|---|
| InfoSheet | M4000InfoSheetPDF |
| Brochures | PI3K-Akt-mTORCPathwayBooklet |
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BurkeJF,SchlosserL,HarrisonAD,etal.MK-2206CausesGrowthSuppressionandReducesNeuroendocrineTumorMarkerProductioninMedullaryThyroidCancerThroughAktInhibition.AnnSurgOncol.2013Nov;20(12):3862-8.PMID:23900743.
JiaoP,ZhouYS,YangJX,etal.MK-2206inducescellcyclearrestandapoptosisinHepG2cellsandsensitizesTRAIL-mediatedcelldeath.MolCellBiochem.2013Jun25.[Epubaheadofprint]PMID:23797319.
JinR,NakadaM,TengL,etal.CombinationtherapyusingNotchandAktinhibitorsiseffectiveforsuppressinginvasionbutnotproliferationingliomacells.NeurosciLett.2013Feb8;534:316-21.PMID:23262078.
QuayleSN,LeeJY,CheungLW,etal.SomaticmutationsofPIK3R1promotegliomagenesis.PLoSOne.2012;7(11):e49466.PMID:23166678.
IidaM,BrandTM,CampbellDA,etal.TargetingAKTwiththeallostericAKTinhibitorMK-2206innon-smallcelllungcancercellswithacquiredresistancetocetuximab.CancerBiolTher.2013Jun;14(6):481-91.PMID:23760490.
DaviesBR,GreenwoodH,DudleyP,etal.PreclinicalpharmacologyofAZD5363,aninhibitorofAKT:pharmacodynamics,antitumoractivity,andcorrelationofmonotherapyactivitywithgeneticbackground.MolCancerTher.2012Apr;11(4):873-87.PMID:22294718.
ChengY,ZhangY,ZhangL,etal.MK-2206,anovelallostericinhibitorofAkt,synergizeswithgefitinibagainstmalignantgliomaviamodulatingbothautophagyandapoptosis.MolCancerTher.2012Jan;11(1):154-64.PMID:22057914.
