RAD51-Inhibitor-B02-B02-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemERAD51InhibitorB02Cat.No.:HY-101462CASNo.:1290541-46-6Synonyms:B02分⼦式:C₂₂H₁₇N₃O分⼦量:339.39作⽤靶点:RAD51;Apoptosis作⽤通路:CellCycle/DNADamage;Apoptosis储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:≥37mg/mL(109.02mM)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制备储备液1mM2.9465mL14.7323mL29.4646mL5mM0.5893mL2.9465mL5.8929mL10mM0.2946mL1.4732mL2.9465mL请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。储备液的保存⽅式和期限：-80°C,6months;-20°C,1month。-80°C储存时，请在6个⽉内使⽤，-20°C储存时，请在1个⽉内使⽤。体内实验请根据您的实验动物和给药⽅式选择适当的溶解⽅案。以下溶解⽅案都请先按照InVitro⽅式配制澄的储备液，再依次添加助溶剂：(为保证实验结果的可靠性，澄的储备液可以根据储存条件，适当保存；体内实验的⼯作液，建议您现⽤现配，当天使⽤；以下溶剂前显⽰的百分⽐指该溶剂在您配制终溶液中的体积占⽐；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的⽅式助溶)1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE1.请依序添加每种溶剂：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2mg/mL(5.89mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2mg/mL(5.89mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性RAD51InhibitorB02(B02)⼈RAD51的抑制剂，IC50值为27.4μM。IC50&TargetIC50:27.4μM(hRAD51)[1]体外研究RAD51InhibitorB02specificallyinhibitshumanRAD51(IC50=27.4μM),butnotitsE.colihomologueRecA(IC50>250μM)[1].ThecombinationofB02withcisplatinhasthestrongestkillingeffectonthehumanbreastcancercellsMDA-MB-231[2].体内研究B02significantlyenhancesthetherapeuticeffectofcisplatinontumorcellsinvivo.B02istoleratedbymiceatdosesupto50mg/kgwithoutobviousbodyweightloss.NoinhibitionoftumorgrowthisobservedonmicesolelytreatedbyB02.Micetreatedwith4mg/kgcisplatin,however,showsa33%inhibitionoftumorgrowth.Finally,micetreatedwith50mg/kgB02and4mg/kgcisplatinshowsa66%inhibitionoftumorgrowth[2].PROTOCOLCellAssay[2]Thecellsareexposedfor1h,thenthecellsareishedbyPBSthreetimesandrefreshedbythemediacontainingB02(5µM).After7-10days,cellsarefixedandstainedwithstainingsolution(0.05%crystalviolet,50%methanolinPBS);finallycellcoloniesarecounted[2].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.AnimalMice:CisplatinandB02aredissolvedinNSandcremophor/DMSO/NS(1:1:3)vehicle,respectively,Administration[2]immediatelybeforeinjection.Inacombinationtreatmentgroup,themiceareinjectedwithB02(50mg/kgorindicatedotherwise)andcisplatin(4mg/kgorindicatedotherwise).InB02group,miceareinjectedwithB02andNS;incisplatingroup,miceareinjectedwithcisplatinandB02vehicle.Cisplatin(orNS)isadministrated3hafterB02(oritsvehicle)injection.AllthetreatmentsareexecutedthroughI.P.injectionsonday11,13,15and17aftertumorcellsinoculations[2].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.户使⽤本产品发表的科研⽂献•CancerLett.2021Aug10;S0304-3835(21)00395-5.•Cancers(Basel).2021Apr21;13(9):1998.•JMolMed(Berl).2019Aug;97(8):1183-1193.•JCancerResTher.2020;16(2):215-221.2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemESeemorecustomervalidationsonwww.MedChemEREFERENCES[1].HuangF,etal.IdentificationofspecificinhibitorsofhumanRAD51recombinaseusinghigh-throughputscreening.ACSChemBiol.2011Jun17;6(6):628-35.[2].HuangF,etal.AsmallmoleculeinhibitorofhumanRAD51potentiatesbreastcancercellkillingbytherapeuticagentsinmousexenografts.PLoSOne.2014Jun27;9(6):e100993.McePdfHeightCaution:Produc