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PotentPARPinhibitor(IC50valuesare2,5and200nMforPARP2,PARP1andPARP3,respectively).ExhibitsanticancereffectsinBRCA1mutant,butnotwild-typebreastcancercelllinesinvitro.Inhibitsgrowthofolaparib-resistantmammarytumorsinamousemodelandisapoorsubstratefortheP-gptransporter.Orallybioavailable.
Thetechnicaldataprovidedaboveisforguidanceonly.ForbatchspecificdatarefertotheCertificateofAnalysis.
AllTocrisproductsareintendedforlaboratoryresearchuseonly.
Thefollowingdataisbasedontheproductmolecularweight395.43.Batchspecificmolecularweightsmayvaryfrombatchtobatchduetosolventofhydration,whichwillaffectthesolventvolumesrequiredtopreparestocksolutions.
Referencesarepublicationsthatsupporttheproducts'biologicalactivity.
OplustilO'Connoretal(2016)ThePARPinhibitorAZD2461providesinsightsintotheroleofPARP3inhibitionforbothsyntheticlethalityandtolerABIlitywithchemotherapyinpreclinicalmodels.CancerRes.766084PMID:27550455
Jaspersetal(2013)Lossof53BP1causesPARPinhibitorresistanceinBrca1-mutatedmousemammarytumors.CancerDiscov.368PMID:23103855
Keywords:AZD2461,supplier,AZD2461,potent,PARP,inhibitors,inhibits,poly,(ADP-ribose),polymerases,orally,bioavailable,chemotherapeutics,Poly(ADP-ribose),Polymerase,Poly(ADP-ribose),Polymerase,TocrisBioscience
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