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MK-2206isanorallybioavailableallostericquinolinotriazoloneinhibitoroftheserine/threonineproteinkinaseAkt.ItisselectivelypotentforAkt1,Akt2,andAkt3at5nM,12nM,and65nM,respectively.MK-2206inhibitsauto-phosphorylationofAkt1/2atpositionT308andS473.
CombinationstudieswithEGFRinhibitors(e.g.erlotinibandlapatinib)incancercelllineshaveshownsynergisticeffectsinadose-dependentmanner[1],inhibitingbothPI3KandRas/Erkpathways.RecentstudiesindicatethatbreastcancercelllineswithPTENlossand/orPIK3CAmutationswerealsomoresensitivetoMK-2206[3],andthattargetingeEF-2kinaseinconjunctionwithAktcanalsoenhanceitsantitumoreffect[2].
Technicalinformation:
| ChemicalFormula: | C25H21N5O.2HCl | |
| CAS#: | 1032350-13-2 | |
| MolecularWeight: | 480.39 | |
| Purity: | >98% | |
| Appearance: | BrightYellow | |
| ChemicalName: | 8-(4-(1-aminocyclobutyl)phenyl)-9-phenyl-[1,2,4]triazolo[3,4-f][1,6]naphthyridin-3(2H)-one | |
| Solubility: | Upto20mMinDMSO | |
| Synonyms: | MK-2206,MK2206,MK2206 |
ShippingCondition:Theproductisshippedinaglassvialatambienttemperature.
Storagecondition:Forlongershelflife,storesolidpowderat4oCdesiccated,orstoreDMSOsolutionat-20oC.
Reference:
| 1. | Hiraietal.,MK-2206,anallostericAktinhibitor,enhancesantitumorefficacybystandardchemotherapeuticagentsormoleculartargeteddrugsinvitroandinvivo.MolCancerTher,2010,9(7),1956.PubmedID:20571069 |
| 2. | Liuetal.,RolesofeEF-2kinaseincancer.ChinMedJ2012125(16),2908-2913PubmedID:22932089 |
| 3. | Gonzalez-Anguloetal.,DefiningbioMarkerstopredictsensitivitytoPI3K/Akt/mTORpathwayinhibitorsinbreastcancer.CancerTreatmentRev2012,inpress. |
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