Topo-I-COX-2-IN-1-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemETopoI/COX-2-IN-1Cat.No.:HY-150685分?式:C??H??ClFN?O?分?量:400.83作?靶點:Topoisomerase;ProstaglandinReceptor;Apoptosis作?通路:CellCycle/DNADamage;GPCR/GProtein;Apoptosis儲存?式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY?物活性TopoI/COX-2-IN-1(1H-30)?種潛在的TopoI/COX-2抑制劑，抑制COX-2和TopoI活性的IC50值分別是0.24μM和4.42μM。TopoI/COX-2-IN-1可以誘導(dǎo)細胞凋亡(apoptosis)，抑制癌細胞遷移，具有抗癌活性。IC50&TargetTopoisomeraseICOX-24.42μM(IC50)0.24μM(IC50)體外研究TopoI/COX-2-IN-1(1H-30)(0-100μM,24h)hasanti-tumorcellproliferationactivityandcaninduceapoptosisbyincreasingcaspase-3activityinadose-dependentmanner[1].TopoI/COX-2-IN-1(1H-30)(0.04-0.37μM,48h)showsasignificantdecreaseincellmigrationat0.37μMandreducestheexpressionofMMP-9(matrixmetalloproteinases)inHGC-27andRKOcells[1].TopoI/COX-2-IN-1(1H-30)(10μM,48h)caninhibittheactivationofNF-κBpathwayincancercells[1].CellProliferationAssay[1]CellLine:ColoncancercelllinesHGC-27,RKO,HT-29,SGC-7901,andCT26.WTConcentration:0-100μMIncubationTime:Result:InhibitedtheproliferationofCT26.WT,RKO,HT-29,HGC-27andSGC-7901cellswiththeIC50valuesof3.04,3.12,16.93,4.71and14.95μM,respectively.ApoptosisAnalysis[1]1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemECellLine:HGC-27,RKOcelllinesConcentration:1.1μM,3.3μM,10μMIncubationTime:24hoursResult:Increasedcaspase-3positivecellsto55.94%and69.46%at10μMcomparingto1.08%and9.39%intheuntreatedgroupinRKOandHGC-27cellsrespectively.CellCycleAnalysis[1]CellLine:HGC-27,RKOcelllinesConcentration:1.1μM,3.3μM,10μMIncubationTime:Result:InducedblockedinG2/Mphasesignificantly.體內(nèi)研究TopoI/COX-2-IN-1(1H-30)(intraperitonealinjection,100mg/kg,twiceaday,14days)mayinhibittumorgrowthbyincreasingtheexpressionofcaspase-3anddecreasingMMP-9andCOX-2intumortissuestoinduceapoptosisinBALB/cmicemodelinfectedwithCT26.WTcoloncancercells[1].AnimalModel:BALB/cmicemodelinfectedwithCT26.WTcoloncancercells[1]Dosage:100mg/kgAdministration:Intraperitonealinjection;twiceaday;14daysResult:Significantreductionintumorsizeandtumorweightandnosignificantdifferencesinbodyweight,organs.AnimalModel:SDrats[1]Dosage:100mg/kgAdministration:Intraperitonealinjection;onceResult:b>ThepharmacokineticparametersofTopoI/COX-2-IN-1(1H-30)ParameterTopoI/COX-2-IN-1(1H-30)t1/21.56hTmax0.67hCmax20.19μg/mLAUC0-t18.20mg/L?hAUC0?inf_obs18.60mg/L?hREFERENCES[1].JunfangLi,etal.N-2-(Phenylamino)BenzamideDerivativesasDualInhibitorsofCOX-2andTopoIDeterGastrointestinalCancersviaTargetingInflammationandTumorProgression.JMedChem.2022Jul22.2/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEMcePdfHeightCaution:Producthasnotbeenfullyvalidatedfor