Anticancer-agent-31-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEAnticanceragent31Cat.No.:HY-143302CASNo.:2222930-72-3分⼦式:C₂₈H₂₁F₂N₅O₂分⼦量:497.5作⽤靶点:Others作⽤通路:Others储存⽅式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY⽣物活性Anticanceragent31⼀种1,3-⼆苯脲喹喔啉衍⽣物，⼀种抗癌剂。Anticanceragent31引起细胞周期在S期阻滞并诱导凋亡(apoptosis)，具有抗肿瘤活性。体外研究Anticanceragent31(compound2d)showsanticanceractivityagainsthumantumorcelllines(MGC-803,NCI-H460,T-24,HeLa,HepG2,andSMMC-7721)anddisplayslowercytotoxicitythan5-FU(HY-90006),Sorafenib(HY-10201),andCisplatin(HY-17394)[1].Anticanceragent31(10,and15μM;24h)arrestscellcycleatSphaseinMGC-803cells,andinducestumorcellsapoptosis[1].Anticanceragent31(5,10,and15μM;24h)reducescellcycleregulatoryproteinCDK2,CDK4,cyclinA2,cyclinB1,andApaf-1,anti-apoptoticproteinBcl-2;increasespro-apoptoticproteinBaxproteinlevel[1].Anticanceragent31(5,10μM;24h)activatescaspase-3andcaspase-9by73.6%and65.3%,respectively;andalsocausesthelossofmitochondrialmembranepotential(MMP)increaseinJC-1(HY-15534)detection[1].CellCytotoxicityAssay[1]CellLine:Normalcellline:HL-7702andsixhumantumorcelllines:MGC-803,NCI-H460,T-24,HeLa,HepG2,andSMMC-7721Concentration:IncubationTime:Result:InhibitedhumantumorcellwithIC50sof9μM(MGC-803),12.3μM(HeLa),13.3μM1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE(NCI-H460),30.4μM(HepG2),17.6μM(SMMC-7721),27.5μM(T-24),respectively.ShowedlowecytotoxicitywithanIC50valueof80.9μM,higherthantheIC50softumorcellcells.WesternBlotAnalysis[1]CellLine:MGC-803Concentration:0,5,10,15μMIncubationTime:24hoursResult:Decreasedcellcycleregulatoryprotein(cyclin-dependentkinase(CDK)2,CDK4,cyclinA2,andcyclinB1)levelsinadose-dependentmanner.Suppressedanti-apoptoticproteinBcl-2expressionandup-regulatedpro-apoptoticproteinBaxlevel.ApoptosisAnalysis[1]CellLine:MGC-803Concentration:0,5,10,15μMIncubationTime:24hoursResult:CausedMGC-803cellsarrestatSphasefrom24.45%to41.39%at15μMconcentration.IndicatedthattherewasainteractionwithDNAinthenucleusandaffectDNAreplication.Increasedthepercentageofapoptotictumorcellsfrom4.31%to37.21%.Immunofluorescence[1]CellLine:MGC-803Concentration:5,10μMIncubationTime:24hours;JC-1asthefluorescentprobeResult:Inducedthelossofmitochondrialmembranepotential(MMP)from0.79%(control)to37.4%(5μM)and81.4%(10μM),respectively.REFERENCES[1].LiGZ,etal.Synthesisandbiologicalevaluationofnovel1,3-diphenylureaquinoxalinederivativesaspotentanticanceragents.MedChemRes30,2021.1496-1511.McePdfHeight2/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemECaution:Producthasnotbeenfullyvalidatedformedi