Pulrodemstat-CC-90011-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEPulrodemstatCat.No.:HY-129388ACASNo.:1821307-10-1Synonyms:CC-90011;LSD1-IN-7分⼦式:C₂₄H₂₃F₂N₅O₂分⼦量:451.47作⽤靶点:HistoneDemethylase作⽤通路:Epigenetics储存⽅式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY⽣物活性Pulrodemstat(CC-90011)⼀种有效的，选择性的，可逆的和具有⼝服活性的赖氨酸特异性脱甲酶-1(LSD1)抑制剂，IC50为0.25nM。Pulrodemstat对LSD2，MOA-A和MAO-B的酶抑制作⽤较⼩。Pulrodemstat诱导急性髓细胞性⽩⾎病(AML)和⼩细胞肺癌(SCLC)细胞分化，并具有有效的抗癌活性。IC50&TargetIC50:0.25nM(LSD1)[1]体外研究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].体内研究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—您⾝边的抑制剂⼤师www.MedChemEandoralbioavailabilityof32%[1].AnimalModel:BALB/cnudemicebearingsmallcelllungcarcinoma(SCLC)[1]Dosage:5mg/kgAdministration:Oraladministration;daily;for30daysResult:Showedatumorgrowthinhibition(TGI)of78%at5mg/kgwithnobodyweightloss.户使⽤本产品发表的科研⽂献•ACSPharmacolTranslSci.November12,2021.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].ToufikeKanouni,etal.DiscoveryofCC-90011:APotentandSelectiveReversibleInhibitorofLysineSpecificDemethylase1(LSD1).JMedChem.2020Dec10;63(23):14522-14529.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forr