1D09C3-生命科学试剂-MCE

Hotline:400-820-3792Inhibitors • ScreeningLibraries • Proteinswww.MedChemE1D09C3Cat.No.:HY-P991590CASNo.:791073-97-7作用靶点:MHC;Apoptosis;JNK作用通路:Immunology/Inflammation;Apoptosis;MAPK/ERKPathway储存方式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY生物活性1D09C3是一种全人源化的抗HLA-DR单克隆抗体。1D09C3通过一系列级联反应诱导细胞凋亡(apoptosis)和死亡，包括活性氧(ROS)产生、JNK激活、线粒体膜去极化以及从线粒体释放AIF。1D09C3在JVM-2细胞和GRANTA-519细胞异种移植瘤小鼠模型中显示出强大的抗肿瘤活性，提高了总体生存率和中位生存期。1D09C3可用于癌症研究，如慢性淋巴细胞白血病(CLL)[1][2][3]。IC50&TargetHLA-DRβ体外研究1D09C3(2.5µg/mL,24h)significantlyreducescellcountingsandcellsurvivalinHLA-DR+,butnotHLA-DR-celllines[1][2].1D09C3(0.1-10µg/mL,4-24h)inducesapotenttime-anddose-dependentdeathofJVM-2andGRANTA-519cells[1].1D09C3(10µg/mL,4-24h)inducescellapoptosisthroughacaspase-independentpathwayinJVM-2andGRANTA-519cells[1].1D09C3(10µg/mL,5-240min)inducesmitochondrialdepolarizationandgenerationofROSinJVM-2andGRANTA-519cells[1].1D09C3(10µg/mL,0.5-4h)inducescelldeathinvolvingactivationoftheJNK[1].1D09C3(2.5µg/mL,4h)inducescelldeathB-CLLcelldeath[1][3].1D09C3(10µg/mL,48h)reducescellcountsby20%foractivatedTcellsandby50%forrestingandactivatedBcells[1].CellProliferationAssay[1]CellLine:HLA-DR+celllinesJVM-2andGRANTA-519andtheHLA-DRcelllineSU-DHL-11/3 MasterofBioactiveMolecules—您身边的抑制剂大师www.MedChemEConcentration:2.5µg/mLIncubationTime:24hResult:Reducedtheabsolutenumberofviablecellsby3-foldand48-fold,andthesurvivaloftumorcellsby33-foldand25-foldforJVM-2andGRANTA-519,respectivelyWesternBlotAnalysis[1]CellLine:JVM-2andGRANTA-519cellsConcentration:10µg/mLIncubationTime:4,18and24hResult:Showednosignificantchangeofcaspase-8,9,3andRARP.WesternBlotAnalysis[1]CellLine:GRANTA-519cellsConcentration:10μg/mLIncubationTime:0.5,1,2and4hResult:UpregulatedthelevelsofJNKinmitochondrialandAIFincytosolic.体内研究1D09C3(0.01-6mg/mouse,i.v.)significantlyincreasesoverallsurvivalandmediansurvivalinJVM-2cellsandGRANTA-519cellsxenograftmicemodels[1].AnimalModel:JVM-2(1x106)cellsxenograftmicemodels(NOD/SCIDmice,6-8weeks)[1]Dosage:0.01mg/mouse(day4),0.1mg/mouse(day4)Administration:IntravenousinjectionResult:Resultedina20%overallsurvivalwithamediansurvivaltimeof64days.AnimalModel:JVM-2(0.25x106)cellsxenograftmicemodels(NOD/SCIDmice,6-8weeks)[1]Dosage:3x1mg/mouse(day4,7,9)and1mg/mouse(day4)fortreatmentofearly-stagedisease;6x1mg/mouseat48-hourintervarsstartingonday15fortreatmentofadvanced-stagediseaseAdministration:IntravenousinjectionResult:Resultedina100%survivalatdoseupto3mg/mouse,anda42%overallsurvivalwitha2/3 MasterofBioactiveMolecules—您身边的抑制剂大师www.MedChemEmediansurvivalof99days.AnimalModel:GRANTA-519cellsandKMS-11cellsxenograftmicemodels(NOD/SCIDmice,6-8weeks)[1][2][3]Dosage:3x1mgmouse(days1,4,and7)fortreatmentofearly-stagediseaseand6x1mg/mouseat48-hourintervarsstartingonday7fortreatmentofadvanced-stagediseaseAdministration:IntravenousinjectionResult:Resultedinasignificantincreaseofmediansurvival(108days),with27%micebeingaliveanddisease-freeattheendofthe120-dayobservationperiodREFERENCESCarlo-StellaC,etal.Theanti-humanleukocyteantigen-DRmonoclonalantibody1D09C3activatesthemitochondrialcelldeathpathwayandexertsapotentantitumoractivityinlymphoma-bearingnonobesediabetic/severecombinedimmunodeficientmice.CancerRes.2006Feb1;66(3):1799-808.Carlo-StellaC,etal.IFN-gammaenhancestheantimyelomaactivityofthefullyhumananti-humanleukocyteantigen-DRmonoclonalantibody1D09C3.CancerRes.2007Apr1;67(7):3269-75.NagyZA,etal.Fullyhuman,HLA-DR-specificmonoclonalantibodiesefficientlyinduceprogrammeddeathofmalignantlymphoidcells.NatMed.2002Aug;8(8):801-7.McePdfH