Pulrodemstat-CC-90011-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEPulrodemstatCat.No.:HY-129388ACASNo.:1821307-10-1Synonyms:CC-90011;LSD1-IN-7分?式:C??H??F?N?O?分?量:451.47作?靶點(diǎn):HistoneDemethylase作?通路:Epigenetics儲(chǔ)存?式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY?物活性Pulrodemstat(CC-90011)?種有效的，選擇性的，可逆的和具有?服活性的賴氨酸特異性脫甲酶-1(LSD1)抑制劑，IC50為0.25nM。Pulrodemstat對(duì)LSD2，MOA-A和MAO-B的酶抑制作?較?。Pulrodemstat誘導(dǎo)急性髓細(xì)胞性??病(AML)和?細(xì)胞肺癌(SCLC)細(xì)胞分化，并具有有效的抗癌活性。IC50&TargetIC50:0.25nM(LSD1)[1]體外研究Pulrodemstat(CC-90011,Compound11)showspotentinductionofon-targetcellulardifferentiationmarkerCD11binTHP-1celllinewithanEC50of7nM,antiproliferativeactivityinAMLkasumi-1cellswithanEC50of2nM[1].SuppressionofGRPisobservedwithtreatmentofPulrodemstat(4days)inadose-dependentmannerandatpharmacologicallyusefulconcentrations(EC50=3nM,H209and4nM,H1417).Pulrodemstat(12days)treatmentofSCLCcellsresultsinpotentantiproliferativeactivity(EC50=6nM,H1417)thatcorrelatedwithGRPsuppression[1].體內(nèi)研究Pulrodemstat(CC-90011;5mg/kg;oraladministration;daily;for30days;for30days)treatmentinhibitstumorgrowthinpatient-derivedxenograftSCLCmodels[1].Pulrodemstat(onceaday;for4days)treatmentresultsinrobustdownregulationofGRPmRNAlevelsat2.5mg/kgandmaximumsuppressionofGRPat5mg/kginaSCLChumantumorxenograft(H1417)mice[1].Afteri.v.administration,Pulrodemstat(Compound11;5mg/kg)hassystemicclearanceof32.4mL/min/kg,eliminationhalf-lifeof2h,andahighvolumeofdistributionof7.5L/kg.Pulrodemstat(Compound11;5mg/kg)isreadilyabsorbedafteroraladministrationwithanAUC0-24hof1.8μM·h,C/sub>maxof0.36μM,1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEandoralbioavailabilityof32%[1].AnimalModel:BALB/cnudemicebearingsmallcelllungcarcinoma(SCLC)[1]Dosage:5mg/kgAdministration:Oraladministration;daily;for30daysResult:Showedatumorgrowthinhibition(TGI)of78%at5mg/kgwithnobodyweightloss.戶使?本產(chǎn)品發(fā)表的科研?獻(xiàn)?ACSPharmacolTranslSci.November12,2021.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].ToufikeKanouni,etal.DiscoveryofCC-90011:APotentandSelectiveReversibleInhibitorofLysineSpecificDemethylase1(LSD1).JMedChem.2020Dec10;63(23):14522-14529.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forr