BM-1197-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEBM-1197Cat.No.:HY-120882CASNo.:1391107-89-3分⼦式:C₅₃H₅₉ClF₄N₆O₇S₄分⼦量:1131.78作⽤靶点:Bcl-2Family作⽤通路:Apoptosis储存⽅式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY⽣物活性BM-1197⼀种有效的和选择性的Bcl-2/Bcl-xL的双重抑制剂，抑制Bcl-2和Bcl-xL的IC50值分别为3.5nM和5.2nM。BM-1197在体外和体内均表现出抗肿瘤作⽤。IC50&TargetBcl-2Bcl-xL3.5nM(IC50)5.2nM(IC50)体外研究BM-1197(2-2000nM;3d)hasmarginalcytotoxicityagainstwild-typemouseembryonicfibroblast(MEF)cellsbutexertspotentgrowth-inhibitoryactivityintheMCL1−/−cells[1].BM-1197showspotentgrowth-inhibitoryactivitiesin7smallcelllungcancer(SCLC)celllineswithIC50s50sof-600nMandweakactivityin2SCLCcelllineswithIC50s>2000nM[1].BM-1197(100nM;16h)potentlyinducesapoptosisinH146cells[1].BM-1197(100nM;2h)disruptstheassociationbetweenBcl-xlandPumaorBiminH146cells[1].BM-1197(100nM;0.5-2h)inducesBaxtranslocation,andit(3-30nM;2h)inducescytochromecreleaseinH146cells[1].CellProliferationAssay[1]CellLine:MEF/MCL1−/−cellsConcentration:2,20,200,2000nMIncubationTime:3daysResult:InhibitedMCL1−/−cellsproliferation.1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEApoptosisAnalysis[1]CellLine:H146cellsConcentration:100nMIncubationTime:16hoursResult:InducedapoptosisinastrictlyBax/Bak-dependentmanner.WesternBlotAnalysis[1]CellLine:H146cellsConcentration:100nMIncubationTime:2hoursResult:AttenuatedtheassociationsbetweenBcl-xLandBimELorPuma.体内研究BM-1197(10mg/kg;i.v.daily5daysperweekfor2weeks)resultsinrapidandcompletetumorregressioninall8miceinH146andH1963tumormodel[1].BM-1197(15mg/kg;i.v.)causesthrombocytopeniainmicebuttheeffectisreversibleevenathighlyefficaciousdoses[1].BM-1197(10mg/kg;i.v.qd)exertsastronganti-tumoreffectandiswelltoleratedinOCI-Ly8xenograftmodels[2].AnimalModel:SCIDmicebearingH146cells[1]Dosage:10mg/kgAdministration:I.v.daily5daysperweekfor2weeksResult:Remainedtumorfreeforatleast32daysaftertheendofthetreatment.REFERENCES[1].BaiL,et,al.BM-1197:anovelandspecificBcl-2/Bcl-xLinhibitorinducingcompleteandlong-lastingtumorregressioninvivo.PLoSOne.2014Jun5;9(6):e99404.[2].SunYL,et,al.AnovelBcl-2inhibitor,BM-1197,inducesapoptosisinmalignantlymphomacellsthroughtheendogenousapoptoticpathway.BMCCancer.2019Dec31;20(1):1.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplication