DDP-38003-trihydrochloride-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEDDP-38003trihydrochlorideCat.No.:HY-19612B分?式:C??H??Cl?N?O分?量:459.84作?靶點:HistoneDemethylase作?通路:Epigenetics儲存?式:4°C,storedundernitrogen*Insolvent:-80°C,6months;-20°C,1month(storedunder

nitrogen)溶解性數(shù)據(jù)體外實驗DMSO:100mg/mL(217.47mM;Needultrasonic)H2O:50mg/mL(108.73mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM2.1747mL10.8733mL21.7467mL5mM0.4349mL2.1747mL4.3493mL10mM0.2175mL1.0873mL2.1747mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；?旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲備液的保存?式和期限：-80°C,6months;-20°C,1month(storedundernitrogen)。-80°C儲存時，請在6個?內(nèi)使?，-20°C儲存時，請在1個?內(nèi)使?。體內(nèi)實驗請根據(jù)您的實驗動物和給藥?式選擇適當(dāng)?shù)娜芙?案。以下溶解?案都請先按照InVitro?式配制澄的儲備液，再依次添加助溶劑：(為保證實驗結(jié)果的可靠性，澄的儲備液可以根據(jù)儲存條件，適當(dāng)保存；體內(nèi)實驗的?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?；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的?式助溶)1.請依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.5mg/mL(5.44mM);Clearsolution2.請依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(5.44mM);Clearsolution1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEBIOLOGICALACTIVITY?物活性DDP-38003trihydrochloride新穎，有?服活性的KDM1A/LSD1抑制劑，IC50值為84nM。IC50&TargetIC50:84nM(KDM1A/LSD1)[1]體外研究DDP-38003inhibitsKDM1AwithanIC50of84nM.DDP-38003ismoreactiveinreducingthecolonyformingabilityandininducingthedifferentiationofTHP-1cellscomparedtothe1R,2Sanalogue[1].體內(nèi)研究DDP-38003exhibitsinvivoefficacyafteroraladministration,determininga62%increasedsurvivalinmouseleukemiamodelswithevidenceofKDM1Ainhibition.ThehalflifeofDDP-38003is8h.AsignificantdosedependentincreaseofmicesurvivalisobtainedbyDDP-38003treatment.Thesurvivalrateincreases35%and62%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:Producthasnotbeenfullyvalidatedformedicalappli