Enavatuzumab-PDL192-DataSheet-生命科学试剂-MCE

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEEnavatuzumabCat.No.:HY-P99361CASNo.:1062149-33-0Synonyms:PDL192;ABT-361;Anti-TNFRSF12A/TWEAKR/CD266ReferenceAntibody(enavatuzumab)作⽤靶点:TNFReceptor作⽤通路:Apoptosis储存⽅式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY⽣物活性Enavatuzumab(PDL192;ABT-361)⼀种⼈化IgG1单克隆抗体，靶向TNF样细胞凋亡弱诱导剂受体(TWEAK)。TWEAK(Fn14;TNFRSF12A)TWEAK受体(TweakR)的天然配体，可刺激多种细胞反应。Enavatuzumab通过直接的TweakR信号和抗体依赖性细胞介导的细胞毒性(ADCC)诱导肿瘤⽣长抑制。Enavatuzumab可以主动募集和激活⾻髓效应细胞来杀死肿瘤细胞。Enavatuzumab在体外和体内抑制各种⼈类TweakR阳性癌细胞系和异种移植物的⽣长。体外研究Enavatuzumab(0.1-1000ng/mL;4hours)induceseffectorcellactivationandtumorcellkillinginvitro[1].Enavatuzumab(10ꢀμg/mL;for24ꢀhours)resultsinsignificantlyincreasedmigrationofimmuneeffectorcellstowardthetumorcellsinSN12CandA375cells[1].CellViabilityAssay[1]CellLine:RenalcarcinomacelllineSN12C,themelanomacelllineA375,thecolorectalcancercelllinesHCT116andDLD-1Concentration:0.1,1,10,100,1000ng/mLIncubationTime:4hoursResult:ShowedpotenttumorcellkillingonallTweakR-positivetumorcellstested.体内研究Enavatuzumab(10ꢀmg/kg;IP;threetimesperweek;7doses)showsdiverseantitumoractivitiesondifferentxenografttumors[1].1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEAnimalModel:6-weekoldSCIDmicewithSN12CorHCT116orDLD-1orA375tumors[1]Dosage:10ꢀmg/kgAdministration:IP;threetimesperweek;6doses(DLD-1model),7doses(SN12Cmodel),9doses(A375orHCT116model)Result:SomeTweakR-expressingcells,suchasSN12CandA375,weresensitiveinvivoandinvitro.SomeTweakR-expressingcelllines,suchasHCT116andDLD-1,werenotsensitivetoenavatuzumabtreatmentinvivo,thoughbothcelllineswereeffectivelykilledviaADCCinvitro.Up-regulatedtheactivationmarkersonsplenocytesinSN12Ctumor-bearingmice.REFERENCES[1].ShimingYe,etal.Enavatuzumab,aHumanizedAnti-TWEAKReceptorMonoclonalAntibody,ExertsAntitumorActivitythroughAttractingandActivatingInnateImmuneEffectorCells.JImmunolRes.2017;2017:5737159.[2].LudmilladePlater,etal.Predictivegenesignatureofresponsetotheanti-TweakRmAbPDL192inpatient-derivedbreastcancerxenografts.PLoSOne.2014Nov6;9(11):e104227.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresea