Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEEnavatuzumabCat.No.:HY-P99361CASNo.:1062149-33-0Synonyms:PDL192;ABT-361;Anti-TNFRSF12A/TWEAKR/CD266ReferenceAntibody(enavatuzumab)作?靶點:TNFReceptor作?通路:Apoptosis儲存?式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY?物活性Enavatuzumab(PDL192;ABT-361)?種?化IgG1單克隆抗體，靶向TNF樣細(xì)胞凋亡弱誘導(dǎo)劑受體(TWEAK)。TWEAK(Fn14;TNFRSF12A)TWEAK受體(TweakR)的天然配體，可刺激多種細(xì)胞反應(yīng)。Enavatuzumab通過直接的TweakR信號和抗體依賴性細(xì)胞介導(dǎo)的細(xì)胞毒性(ADCC)誘導(dǎo)腫瘤?長抑制。Enavatuzumab可以主動募集和激活?髓效應(yīng)細(xì)胞來殺死腫瘤細(xì)胞。Enavatuzumab在體外和體內(nèi)抑制各種?類TweakR陽性癌細(xì)胞系和異種移植物的?長。體外研究Enavatuzumab(0.1-1000ng/mL;4hours)induceseffectorcellactivationandtumorcellkillinginvitro[1].Enavatuzumab(10?μg/mL;for24?hours)resultsinsignificantlyincreasedmigrationofimmuneeffectorcellstowardthetumorcellsinSN12CandA375cells[1].CellViabilityAssay[1]CellLine:RenalcarcinomacelllineSN12C,themelanomacelllineA375,thecolorectalcancercelllinesHCT116andDLD-1Concentration:0.1,1,10,100,1000ng/mLIncubationTime:4hoursResult:ShowedpotenttumorcellkillingonallTweakR-positivetumorcellstested.體內(nèi)研究Enavatuzumab(10?mg/kg;IP;threetimesperweek;7doses)showsdiverseantitumoractivitiesondifferentxenografttumors[1].1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEAnimalModel:6-weekoldSCIDmicewithSN12CorHCT116orDLD-1orA375tumors[1]Dosage:10?mg/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