MPT0B014-6-3-4-5-Trimethoxybenzoyl-quinoline-DataSheet-生命科學(xué)試劑-MCE

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEMPT0B014Cat.No.:HY-120786CASNo.:1215208-59-5Synonyms:6-(3′,4′,5′-Trimethoxybenzoyl)quinoline分?式:C??H??NO?分?量:323.34作?靶點:Microtubule/Tubulin;Apoptosis作?通路:CellCycle/DNADamage;Cytoskeleton;Apoptosis儲存?式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY?物活性MPT0B014?種微管蛋?聚合(tubulinpolymerization)抑制劑。MPT0B014誘導(dǎo)癌細(xì)胞凋亡(apoptosis)。MPT0B014可?于癌癥研究。IC50&TargetTubulinpolymerization[1]體外研究MPT0B014(0-1μM;48h)inhibitsA549,H1299andH226cellsgrowthinadose-dependentmanner[1].MPT0B014(0.05-0.3μM;24and48h)arrestscellcycleatG2/Mandsub-G1phasesandinducesapoptosisinA549cells[1].CellViabilityAssay[1]CellLine:A549,H1299,H226andHUVECcellsConcentration:0,0.025,0.05,0.075and1μMIncubationTime:48hResult:InhibitedcellviabilitywithIC50sof0.109±0.01,0.055±0.004,0.077±0.005and0.536±0.166μMagainstA549,H1299,H226andHUVECcells,respectively.CellCycleAnalysis[1]CellLine:A549,H1299andH2261/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEConcentration:0.05,0.1and0.3μMIncubationTime:24and48hResult:Treatmentfor24hledtonotableaccumulationofcellsintheG2/Mphase.At48h,sub-G1apoptoticcellpopulationswereincreasedinaconcentration-dependentmanner.CellsintheG2/Mphasebegantoriseat12hpost-treatmentandpeakedat24h.Followingthis,therewasanemergenceofcellsinthesub-G1populationphaseuntil48h.WesternBlotAnalysis[1]CellLine:A549,H1299andH226Concentration:0.05,0.1and0.3μMIncubationTime:24hResult:ResultedinamarkedincreaseinexpressionofthemitosismarkerMPM2andtheproteinscyclinB1,Cdc2,Thr161,AuroraAandAuroraBinaconcentration-dependentmanner.DecreasedtheexpressionofCdc(Tyr15)andCdc25C,whereastotalproteinlevelsofCdc2didnotchange.ApoptosisAnalysis[1]CellLine:A549Concentration:0.05,0.075,0.1and0.3μMIncubationTime:48hResult:Inducedapoptosisinaconcentration-dependentmanner.WesternBlotAnalysis[1]CellLine:A549Concentration:0.05,0.1and0.3μMIncubationTime:24,36and48hResult:Inducedactivationofcaspases-3,-7,-8and-9,andcleavageofPARPinatime-andconcentration-dependentmanner.SignificantlyinducedBcl-2phosphorylation.Down-regulatedMcl-1expressioninaconcentration-dependentmanner.體內(nèi)研究ThecombinationofMPT0B014(100mg/kg;i.v./i.p.;dailyfor25days)and25mg/kgErlotinib(HY-50896)significantlyimprovesA549tumorinhibitioninmice[1].2/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEAnimalModel:Nudeathymicmice,A549xenografts[1]Dosage:100mg/kgaloneorincombinationwith25mg/kgErlotinib(HY-50896)Administration:i.v./i.p.,dailyfor25daysResult:Thecombinedtreatmentresultedinmoresignificanttumorgrowthdelay(28%)comparedwithtreatmentalone(7%).Thecombinationproducedsignificantlyhigheranti-tumoractivity.ThegrowthofA549cancercellxenograftswassuppressedby11,21and49%(tumorgrowthinhibition)aftertreatmentwithMPT0B014,ErlotinibandMPT0B014plusErlotinib,respectively.REFERENCES[1].TsaiAC,etal.Invitroandinvivoanti-tumoureffectsofMPT0B014,anovelderivativearoylquinoline,andincombinationwitherlotinibinhumannon-small-celllungcancercells.BrJPharmacol.2014Jan;171(1):122-33.McePdfHeightCaution:Producthasnot