MMAF-d8-hydrochloride-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEMMAF-d8hydrochlorideCat.No.:HY-15579AS分⼦式:C₃₉H₅₈D₈ClN₅O₈分⼦量:776.47作⽤靶点:Microtubule/Tubulin;ADCCytotoxin作⽤通路:CellCycle/DNADamage;Cytoskeleton;Antibody-drugConjugate/ADCRelated储存⽅式:4°C,sealedstorage,awayfrommoisture*该产品在溶液状态不稳定，建议您现⽤现配，即刻使⽤。溶解性数据体外实验DMSO:100mg/mL(128.79mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM1.2879mL6.4394mL12.8788mL5mM0.2576mL1.2879mL2.5758mL10mM0.1288mL0.6439mL1.2879mL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；该产品在溶液状态不稳定，建议您现⽤现配，即刻使⽤.BIOLOGICALACTIVITY⽣物活性D8-MMAFhydrochlorideMMAFhydrochloride的氘代形式。IC50&TargetAuristatin体外研究MMAFshowsinvitrocytotoxicityagainstapanelofcelllines.TheIC50valuesforKarpas299,H3396,786-OandCaki-1are119,105,257,and200nM,respectively.TargetedMMAFismuchmorepotentthanthefreedrug,andthatcAC10conjugatesofMMAFdisplaypronouncedactivities.Onamolarbasis,thecAC10-L1-MMAF4isanaverageofover2200-foldmorepotentthanfreeMMAFandisactiveonalltheCD30-positivecelllinestested[1].1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE体内研究ThemaximumtolerateddoseinmiceofMMAF(>16mg/kg)ismuchhigherthanMMAE(1mg/kg).cAC10-L1-MMAF4hasanMTDof50mg/kginmiceand15mg/kginrats.ThecorrespondingcAC10-L4-MMAF4ADCwasmuchlesstoxic,havingMTDsinmiceandratsof>150mg/kgand90mg/kginrats,respectively[1].PROTOCOLCellAssay[1]Cellsaretreatedwithserialdilutionsoftestmoleculesandincubated4-6daysdependingoncellline.AssessmentofcellulargrowthanddatareductiontogenerateIC50valuesisdoneusingAlamarBluedyereductionassay[1].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.AnimalMice:WhensubcutaneousKarpas299tumorsizereaches300mm3,threeanimalspergroupreceivesoneAdministration[1]injectionof10mgantibodycomponent/kgbodyweightofeithercAC10-L1-MMAF4orcBR96-L1-MMAF4intravenously.Tumorsarethenremovedandplacedinoptimalcuttingtemperaturecompound,and5μm-thinfrozentissuesectionsarestainedusingimmunohistochemistryevaluation[1].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.户使⽤本产品发表的科研⽂献•TechnischeUniversitätDarmstadt.05Aug2022.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].DoroninaSO,etal.EnhancedactivityofmonomethylauristatinFthroughmonoclonalantibodydelivery:effectsoflinkertechnologyonefficacyandtoxicity.BioconjugChem.2006Jan-Feb;17(1):114-24.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplica