AZD5582-dihydrochloride-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEAZD5582dihydrochlorideCat.No.:HY-110346CASNo.:1883545-51-4分⼦式:C₅₈H₈₀Cl₂N₈O₈分⼦量:1088.21作⽤靶点:IAP;Apoptosis作⽤通路:Apoptosis储存⽅式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY⽣物活性AZD5582dihydrochlorideIAP拮抗剂，可以有效与cIAP1，cIAP2和XIAP的BIR3结构域结合,IC50值分别为15，21，15nM。AZD5582诱导凋亡(apoptosis)[1]。IC50&TargetcIAP1cIAP2XIAP15nM(IC50)21nM(IC50)15nM(IC50)体外研究AZD5582(20nM;48hours)inhibitscellviabilitybycooperationwithIFNγorviraldouble-strandedRNA(dsRNA)inH1975NSCLCcells[2].AZD5582(20nM;17or25hours)downregulatescIAP-1,activatesRIPK1(upstreamregulatorofcaspase-8),andtriggerstheactivationofextrinsic(caspase-8)andintrinsic(caspase-9)apoptosispathways,causingthecleavageofcaspase-3andcaspase-7[2].AZD5582(20nM;48hours)involvesinapoptosisduetoinductionofcelldeathandactivecaspase-3/8activitiesbyAZD5582andIFNγco-treatmentinHCC827NSCLCcells[2].CellViabilityAssay[2]CellLine:H1975NSCLCcelllineConcentration:20nMIncubationTime:48hoursResult:CooperatedwithIFNγorviraldouble-strandedRNA(dsRNA)toinhibitcellviabilityevencelldeath.ApoptosisAnalysis[2]1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemECellLine:HCC827NSCLCcelllineConcentration:20nMIncubationTime:48hoursResult:HadaninhibitoryeffectoncellviabilitybycooperatingwithIFNγ.WesternBlotAnalysis[2]CellLine:H1975NSCLCcelllineConcentration:20nMIncubationTime:17or25hoursResult:Down-regulatedcIAP-1,activatedRIPK1(upstreamregulatorofcaspase-8),triggeredthecleavage(activation)ofcaspase-3,7,8and9.体内研究AZD5582(intravenousinjection;0.1-3.0mg/kg;onceaweek;2weeks)causesdegradationofcIAP1andcaspase3cleavageintumorcells,andafteratwo-weektreatment,thetumorslargelyresolved;whenthemicearegivenamediumdose(0.5mg/kg)ofAZD5582,cIAP1degradesafteradministration,butittakesawhiletimetoreachapoptosis-inducingeffect[1].AnimalModel:MDA-MB-231xenograft-bearingmice[1]Dosage:0.1mg/kg,0.5mg/kg,3.0mg/kgAdministration:Intravenousinjection;onceaweek;2weeksResult:ResultedincIAP1degradationandcaspase-3cleavagewithintumorcellsandcausessubstantialtumorregressionsfollowingtwoweeklydosesof3.0mg/kg户使⽤本产品发表的科研⽂献•MaterSciEngCMaterBiolAppl.29December2021,112615.•BiochimBiophysActaMolBasisDis.2019Jun26;1865(10):2618-2632.•CellSignal.2020Aug;72:109654.•ResearchSquarePreprint.2021May.Seemorecustomervalidationsonwww.MedChemEREFERENCES2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE[1].HennessyEJ,etal.DiscoveryofanovelclassofdimericSmacmimeticsaspotentIAPantagonistsresultinginaclinicalcandidateforthetreatmentofcancer(AZD5582).JMedChem.2013Dec27;56(24):9897-919.[2].QinHao,etal.IF-γandSmacmimeticssynergizetoinduceapoptosisoflungcancercellsinaTNFα-independentmanner,CancerCellInt.2018;18:84.McePdfHeightCaution:Producthasnotbeenfullyvalid