DDP-38003-dihydrochloride-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEDDP-38003dihydrochlorideCat.No.:HY-19612ACASNo.:1831167-98-6分⼦式:C₂₁H₂₈Cl₂N₄O分⼦量:423.38作⽤靶点:HistoneDemethylase作⽤通路:Epigenetics储存⽅式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.溶解性数据体外实验DMSO:≥29mg/mL(68.50mM)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制备储备液1mM2.3619mL11.8097mL23.6194mL5mM0.4724mL2.3619mL4.7239mL10mM0.2362mL1.1810mL2.3619mLBIOLOGICALACTIVITY⽣物活性DDP-38003dihydrochloride具有⼝服活性的KDM1A/LSD1抑制剂，IC50值为84nM。IC50&TargetKDM1/LSD1体外研究DDP-38003inhibitsKDM1AwithanIC50of84nM.DDP-38003ismoreactiveinreducingthecolonyformingabilityandininducingthedifferentiationofTHP-1cellscomparedtothe1R,2Sanalogue[1].体内研究DDP-38003exhibitsinvivoefficacyafteroraladministration,determininga62%increasedsurvivalinmouseleukemiamodelswithevidenceofKDM1Ainhibition.ThehalflifeofDDP-38003is8h.AsignificantdosedependentincreaseofmicesurvivalisobtainedbyDDP-38003treatment.Thesurvivalrateincreases35%1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEand62%atthedoseof11.25and22.50mg/kg,respectively.DDP-38003isapotentialoralanticanceragent[1].PROTOCOLAnimalMice:CD-1miceisusedinthestudy.DDP-38003isdissolved(40%PEG400ina5%glucosesolution)andAdministration[1]orallyadministered3daysperweek(Monday,TuesdayandWednesday)for3weeksatthedosesof11.25mg/kgand22.5mg/kg.Thetreatmentstartedonceblastcellsaredetectedintherecipients'peripheralblood(10daysaftercellinjection).ThesurvivalofmiceofthedifferentexperimentalgroupsisanalyzedandrepresentedbyaKaplan-Meiersurvivalplot[1].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.REFERENCES[1].VianelloP,etal.DiscoveryofaNovelInhibitorofHistoneLysine-SpecificDemethylase1A(KDM1A/LSD1)asOrallyActiveAntitumorAgent.JMedChem.2016Feb25;59(4):1501-17.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly