MK-2206-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEMK-2206Cat.No.:HY-108232CASNo.:1032349-77-1分?式:C??H??ClN?O分?量:443.93作?靶點(diǎn):Akt;Autophagy;Apoptosis作?通路:PI3K/Akt/mTOR;Autophagy;Apoptosis儲(chǔ)存?式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY?物活性MK-2206?種具有?服活性的，?效選擇性的，變構(gòu)Akt抑制劑，對(duì)Akt1、Akt2和Akt3中的IC50分別為8、12和65nM。許多乳腺癌細(xì)胞系、PIK3CA突變體和PTEN丟失細(xì)胞系對(duì)MK-2206敏感。具有抗癌活性。IC50&TargetAkt1Akt2Akt38nM12nM65nM體外研究MK-2206(0-10μM;72and96hours)inhibitsthenasopharyngealcarcinoma(NPC)celllinesCNE-1,CNE-2,HONE-1,andSUNE-1proliferationindose-andtime-dependentmanner[3].MK-2206(0-10μM;24and48hours)resultsinadose-dependentincreaseinthepercentageofcellsinG0/G1phaseandaconcomitantreductionofcellnumbersinSphaseinCNE-2andHONE-1cells[3].MK-2206(0-10μM;24hours)attenuatesphosphorylationlevelsofPRAS40andS6inadose-dependentmanner.MK-2206doesnotaffectphosphorylationofGSKα/βandAKT[3].MK-2206(0-10μM;24hours)increasestheappearanceofLC3-IIinCNE-2cellsdose-dependently.Microtubule-associatedprotein1LC3isanessentialautophagyprotein[3].CellProliferationAssay[3]CellLine:TheNPCcelllinesCNE-1,CNE-2,HONE-1,andSUNE-1Concentration:0.08,0.16,0.31,0.63,1.25,2.5,5,10μMIncubationTime:72and96hoursResult:At72and96hours,theIC50valuesinCNE-1,CNE-2,andHONE-1celllineswere3-5μ1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEM,andinSUNE-1,theywerelessthan1μM.CellCycleAnalysis[3]CellLine:CNE-2andHONE-1cellsConcentration:0.625,1.25,2.5,5,10μMIncubationTime:24or48hoursResult:InducedcellcyclearrestatG1inadose-dependentmanner.WesternBlotAnalysis[3]CellLine:SUNE-1andCNE-2cellsConcentration:0.625,1.25,2.5,5,10μMIncubationTime:24hoursResult:InhibitedphosphorylationofAKTdownstreamtargets.CellAutophagyAssay[3]CellLine:CNE-2cellsConcentration:0.625,1.25,2.5,5,10μMIncubationTime:24hoursResult:Inducedautophagy.體內(nèi)研究BothMK-2206doses(oralgavage;480mg/kgonceaweekand240mg/kgthreetimesaweek;for2weeks)caninhibitthegrowthofhumanCNE-2xenograftsinnudemice.Nootherobvioustoxicityisobservedinmice[3].MK-2206(orally;120mg/kg;alternatedays;for3weeks)significantlyinhibitstumorgrowthin3-5weekoldathymicnudemicewithGEOcoloncarcinomacells[4].AnimalModel:Four-to6-week-oldmaleBALB/cnudemicewithCNE-2xenografts[3]Dosage:240mg/kgand480mg/kgAdministration:Oralgavage;240mg/kgforthreetimesaweek;480mg/kgforonceaweek;for2weeksResult:BothdosesinhibitedthegrowthofhumanCNE-2xenograftsinnudemice.戶使?本產(chǎn)品發(fā)表的科研?獻(xiàn)2/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE?Nature.2018Aug;560(7719):499-503.?Cell.2014Feb13;156(4):771-85.?CancerCell.2018Jun11;33(6):1061-1077.e6.?MolCancer.2019Nov21;18(1):167.?CellStemCell.2019Dec5;25(6):754-767.e9.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].XingY,etal.PhaseIItrialofAKTinhibitorMK-2206inpatientswithadvancedbreastcancerwhohavetumorswithPIK3CAorAKTmutations,and/orPTENloss/PTENmutation.BreastCancerRes.2019Jul5;21(1):78.[2].ZhaoYY,etal.EffectsofanoralallostericAKTinhibitor(MK-2206)onhumannasopharyngealcancerinvitroandinvivo.DrugDesDevelTher.2014Oct10;8:1827-37.[3].AgarwalE,etal.AktinhibitorMK-2206promotesanti-tumoractivityandcelldeathbymodulationofAIFandEzrinincolorectalcancer.BMCCancer.2014Mar1;14:145.[4].LiYan,etal.Abstract#DDT01-1:MK-2206:ApotentoralallostericAKTinhibitor.2009.McePdfHeightCaution:P