Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEMelflufenCat.No.:HY-105019CASNo.:380449-51-4Synonyms:Melphalanflufenamide分?式:C??H??Cl?FN?O?分?量:498.42作?靶點(diǎn):DNAAlkylator/Crosslinker;Apoptosis作?通路:CellCycle/DNADamage;Apoptosis儲存?式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY?物活性Melflufen(Melphalanflufenamide)，Melphalan的?種?肽前體藥物，?種烷化劑。Melflufen對多發(fā)性?髓瘤細(xì)胞具有抗腫瘤活性，并抑制?管?成。Melflufen對?髓瘤細(xì)胞DNA不可逆損傷及細(xì)胞毒作?。體外研究Melflufen(Melphalanflufenamide)(0.5-10μM;24hours)decreasesviabilityofMM.1S,INA-6,RPMI-8226,MM.1R,Dox-40,ARP-1,andANBL-6cellsinaconcentration-dependentmanner[1].MelflufeninducesapoptosisinMM.1Scells[1].Melphalanalsoisapotentactivatorofexosomesecretion[3].CellViabilityAssayCellLine:Multiplemyelomacells:MM.1S,INA-6,RPMI-8226,MM.1R,Dox-40,ARP-1,ANBL-6cellsConcentration:0.5,1,3,5,10μMIncubationTime:24hoursResult:Asignificantconcentration-dependentdecreaseinviabilityofallcelllineswasobserved.體內(nèi)研究Melflufen(Melphalanflufenamide)(3mg/kg;i.v.;twice-weeklyfortwoweeks)showsanti-MMactivityinxenograftmousemodel[1].1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEAnimalModel:CB-17SCIDmice(humanplasmacytomaMM.1Sxenograftmousemodel)[1]Dosage:3mg/kgAdministration:I.v.;twice-weeklyfortwoweeksResult:SignificantlyinhibitedMMtumorgrowthandprolongedsurvivalofmice.REFERENCES[1].ChauhanD,etal.Invitroandinvivoantitumoractivityofanovelalkylatingagent,melphalan-flufenamide,againstmultiplemyelomacells.ClinCancerRes.2013;19(11):3019-3031.[2].RayA,etal.AnovelalkylatingagentMelflufeninducesirreversibleDNAdamageandcytotoxicityinmultiplemyelomacells.BrJHaematol.2016;174(3):397-409.[3].McAndrewsKM,et,al.Mechanismsassociatedwithbiogenesisofexosomesincancer.MolCancer.2019Mar30;18(1):52.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly.Tel:40