Annexuzlimab-MDX-124-生命科学试剂-MCE

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEAnnexuzlimabCat.No.:HY-P991864Synonyms:MDX-124作⽤靶点:FormylPeptideReceptor(FPR)作⽤通路:GPCR/GProtein储存⽅式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY⽣物活性Annexuzlimab⼀种⼈化IgG1单克隆抗体，可特异性结合ANXA1，从⽽⼲扰其与甲酰肽受体1和2(FPR1/2)的相互作⽤。Annexuzlimab阻滞细胞周期进程，导致癌细胞在G1期累积。Annexuzlimab靶向分泌的ANXA1，阻⽌FPR1/2的激活，从⽽减少癌症进展。Annexuzlimab可⽤于三性乳腺癌、胰腺癌和⾻⾁瘤的研究。IC50&TargetAnnexinA1/ANXA1体外研究Annexuzlimab(MDX-124)(2.5-10μM;72h)significantlyreducesproliferationinadose-dependentmannerinANXA1-expressinghumancancercelllines,with10μMcausing>50%viabilityreductioninsomebreastandovariancelllines,buthasnoeffectonnon-ANXA1-expressinglungcancercelllines[1].Annexuzlimab(10-25μM;24h)inducesadose-dependentG1phasecellcyclearrest,with25μMcausingthemostpronouncedeffects(33.5%G1increaseinMDA-MB-231,21.2%inA549,10.8%inBxPC-3),anddoesnotinduceapoptosis[1].Annexuzlimab(5μM;72h)doesnotinduceapoptosisinMCF-7breastorCaco-2colorectalcancercells[1].Annexuzlimabincubationofosteosarcomacelllinessignificantlyinhibitscellgrowththroughdose-dependentcellcyclearrestandalsosignificantlyreducesthemigrationabilityofosteosarcomacellline[2].CellProliferationAssay[1]CellLine:MCF-7,HCC1806,MDA-MB-231,MCF-7/TAMR7,BxPC-3,MIAPaCa-2,PANC-1,A2780,A2780cis,A2780ADR,Caco-2,HCT116,SW480,NCI-H69/CPR,A549,COR-L23,COR-L23.5010Concentration:2.5-10μM1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEIncubationTime:72hResult:Causedasignificantdose-dependentreductionincellularproliferationinallANXA1-expressingbreast,pancreatic,ovarian,colorectal,andsomelungcancercelllinescomparedtoIgG1isotypecontrol;At10μM,MCF-7,HCC1806,andMDA-MB-231had>50%viabilityreduction,MCF-7/TAMR7had21%reduction,BxPC-3had40%reduction,MIAPaCa-2had20%reduction,PANC-1had34%reduction,A2780had31%reduction,A2780cishad48%reduction,A2780ADRhad72%reduction,Caco-2,HCT116,andSW480hadsignificantreduction,NCI-H69/CPRhad36%reduction,A549had37%reduction;Showednoanti-proliferativeactivityinnon-ANXA1-expressingCOR-L23andCOR-L23.5010lungcancercells.CellCycleAnalysis[1]CellLine:BxPC-3,MIAPaCa-2,MDA-MB-231,A549Concentration:10μM,25μMIncubationTime:24hResult:Inducedadose-dependentG1phasecellcyclearrestcomparedtountreatedcontrolcells;At25mM,MDA-MB-231hada33.5%increaseinG1phaseand29.1%decreaseinSphase,A549hada21.2%increaseinG1phaseand18.3%decreaseinSphase,BxPC-3hada10.8%increaseinG1phaseand10.4%decreaseinSphase;Didnotinduceapoptosis(nosubG0/G1peakobserved).ApoptosisAnalysis[1]CellLine:MCF-7,Caco-2Concentration:5μMIncubationTime:72hResult:Showednosignificantdifferenceinthepercentageofearlyorlateapoptotic/necroticcellscomparedtountreatedcontrolcells.体内研究Annexuzlimab(1mg/kg;i.v.;twodosesonday1andday8)inhibitstumourgrowthinBALB/cmicemodeloftriple-negativebreastcancer(withatumourgrowthinhibitionof23%)[1].AnimalModel:BALB/c(female,9weeksold,orthotopicinoculationwith4T1-lucmurinetriple-negativebreastcancercells)[1]Dosage:1mg/kgAdministration:i.v.;twodosesonday1andday82/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEResult:Significantlyinhibitedtumourgrowthversusvehiclecontrol,achieving23%tumourgrowthinhibitionbyday15.Observednonoticeablechangeinbodyweightthroughoutthestudy.REFERENCES[1].Al-AliHN,etal.Atherapeuticantibodytargetingannexin-A1inhibitscancercellgrowthinvitroandinvivo.Oncogene.2024;43(8):608-614.[2].F.Dempsey,etal.1MDX-124,anovelanti-ANXA1antibody,hassignificantanti-canceractivityinpreclinicalmodelsofosteosarcoma.McePdfHeight