RAD51-Inhibitor-B02-B02-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemERAD51InhibitorB02Cat.No.:HY-101462CASNo.:1290541-46-6Synonyms:B02分?式:C??H??N?O分?量:339.39作?靶點(diǎn):RAD51;Apoptosis作?通路:CellCycle/DNADamage;Apoptosis儲(chǔ)存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:≥37mg/mL(109.02mM)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM2.9465mL14.7323mL29.4646mL5mM0.5893mL2.9465mL5.8929mL10mM0.2946mL1.4732mL2.9465mL請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；?旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲(chǔ)備液的保存?式和期限：-80°C,6months;-20°C,1month。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)?內(nèi)使?，-20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)?內(nèi)使?。體內(nèi)實(shí)驗(yàn)請(qǐng)根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥?式選擇適當(dāng)?shù)娜芙?案。以下溶解?案都請(qǐng)先按照InVitro?式配制澄的儲(chǔ)備液，再依次添加助溶劑：(為保證實(shí)驗(yàn)結(jié)果的可靠性，澄的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的?作液，建議您現(xiàn)?現(xiàn)配，當(dāng)天使?；以下溶劑前顯?的百分?指該溶劑在您配制終溶液中的體積占?；如在配制過(guò)程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過(guò)加熱和/或超聲的?式助溶)1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE1.請(qǐng)依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2mg/mL(5.89mM);Clearsolution2.請(qǐng)依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2mg/mL(5.89mM);ClearsolutionBIOLOGICALACTIVITY?物活性RAD51InhibitorB02(B02)?RAD51的抑制劑，IC50值為27.4μM。IC50&TargetIC50:27.4μM(hRAD51)[1]體外研究RAD51InhibitorB02specificallyinhibitshumanRAD51(IC50=27.4μM),butnotitsE.colihomologueRecA(IC50>250μM)[1].ThecombinationofB02withcisplatinhasthestrongestkillingeffectonthehumanbreastcancercellsMDA-MB-231[2].體內(nèi)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.戶使?本產(chǎn)品發(fā)表的科研?獻(xiàn)?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?邊的抑制劑?師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