MMAF-d8-hydrochloride-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEMMAF-d8hydrochlorideCat.No.:HY-15579AS分?式:C??H??D?ClN?O?分?量:776.47作?靶點(diǎn):Microtubule/Tubulin;ADCCytotoxin作?通路:CellCycle/DNADamage;Cytoskeleton;Antibody-drugConjugate/ADCRelated儲(chǔ)存?式:4°C,sealedstorage,awayfrommoisture*該產(chǎn)品在溶液狀態(tài)不穩(wěn)定，建議您現(xiàn)?現(xiàn)配，即刻使?。溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:100mg/mL(128.79mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM1.2879mL6.4394mL12.8788mL5mM0.2576mL1.2879mL2.5758mL10mM0.1288mL0.6439mL1.2879mL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；該產(chǎn)品在溶液狀態(tài)不穩(wěn)定，建議您現(xiàn)?現(xiàn)配，即刻使?.BIOLOGICALACTIVITY?物活性D8-MMAFhydrochlorideMMAFhydrochloride的氘代形式。IC50&TargetAuristatin體外研究MMAFshowsinvitrocytotoxicityagainstapanelofcelllines.TheIC50valuesforKarpas299,H3396,786-OandCaki-1are119,105,257,and200nM,respectively.TargetedMMAFismuchmorepotentthanthefreedrug,andthatcAC10conjugatesofMMAFdisplaypronouncedactivities.Onamolarbasis,thecAC10-L1-MMAF4isanaverageofover2200-foldmorepotentthanfreeMMAFandisactiveonalltheCD30-positivecelllinestested[1].1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE體內(nèi)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.戶使?本產(chǎn)品發(fā)表的科研?獻(xiàn)?TechnischeUniversit?tDarmstadt.05Aug2022.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].DoroninaSO,etal.EnhancedactivityofmonomethylauristatinFthroughmonoclonalantibodydelivery:effectsoflinkertechnologyonefficacyandtoxicity.BioconjugChem.2006Jan-Feb;17(1):114-24.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplica