Tubulin-polymerization-IN-9-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemETubulinpolymerization-IN-9Cat.No.:HY-146718CASNo.:2485020-93-5分⼦式:C₁₉H₁₉NO₅Se分⼦量:420.32作⽤靶点:Microtubule/Tubulin;Apoptosis作⽤通路:CellCycle/DNADamage;Cytoskeleton;Apoptosis储存⽅式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY⽣物活性Tubulinpolymerization-IN-9⼀种有效的微管蛋⽩(tubulin)抑制剂，IC50为1.82μM。Tubulinpolymerization-IN-9能引起细胞周期阻滞在G2/M期，诱导K562细胞凋亡(apoptosis)和线粒体去极化。Tubulinpolymerization-IN-9具有强效的抗⾎管和抗肿瘤活性[1]。IC50&TargetIC50:1.82μM(tubulin)[1]体外研究Tubulinpolymerization-IN-9(compound11k)(0.1,1,10μM;72hours)haspotentactivityagainstthesethreecancercelllineswithIC50valuesrangingfrom0.287to0.621μM[1].Tubulinpolymerization-IN-9(0.15,0.3and0.6μM;24hours)inducesadose-dependentcollapseofthemicrotubulenetworks[1].Tubulinpolymerization-IN-9(0.15,0.3and0.6μM;48hours)observesagradualaccumulationofcellsatG2/MphaseinK562cells[1].Tubulinpolymerization-IN-9(0.15,0.3and0.6μM;72hours)effectivelyinducescellapoptosisinK562cellsinaconcentration-dependentmanner[1].Tubulinpolymerization-IN-9(0.15,0.3and0.6μM;24hours)causesmitochondrialdepolarizationofK562cellsintheprocessofapoptosis[1].CellProliferationAssayCellLine:K562HepG2andHCT-8cells[1]Concentration:0.1,1,10μMIncubationTime:72hours1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEResult:ShowedpotentactivityagainstthesethreecancercelllineswithIC50valuesrangingfrom0.287to0.621μM.ImmunofluorescenceCellLine:K562cells[1]Concentration:0.15,0.3and0.6μMIncubationTime:24hoursResult:Inducedadose-dependentcollapseofthemicrotubulenetworks.CellCycleAnalysisCellLine:K562cells[1]Concentration:0.15,0.3and0.6μMIncubationTime:48hoursResult:ObservedagradualaccumulationofcellsatG2/MphaseinK562cells.ApoptosisAnalysisCellLine:K562cells[1]Concentration:0.15,0.3and0.6μMIncubationTime:72hoursResult:EffectivelyinducedcellapoptosisinK562cellsinaconcentration-dependentmanner.体内研究Tubulinpolymerization-IN-9(15and30mg/kg;IV;onceaday,for21days)effectivelysuppressesthetumorvolumeandreducestumorweightby71.1%atadoseof30mg/kg[1].AnimalModel:MaleICRmice(5weeks;injectedwithH22cells;n=6)[1]Dosage:15and30mg/kgAdministration:IV;onceaday,for21daysResult:Effectivelysuppressedthetumorvolumeandreducedtumorweightby71.1%atadoseof30mg/kg.REFERENCES2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE[1].ZhuH,SunH,LiuY,etal.Design,synthesisandbiologicalevaluationofvinylselenonederivativesasnovelmicrotubulepolymerizationinhibitors.EurJMedChem.2020;207:112716.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedica