Hotline:400-820-3792Inhibitors ? ScreeningLibraries ? Proteinswww.MedChemE4SC-207Cat.No.:HY-111251CASNo.:871015-11-1分子式:C??H??N?O?S分子量:382.44作用靶點(diǎn):Microtubule/Tubulin;Apoptosis作用通路:CellCycle/DNADamage;Cytoskeleton;Apoptosis儲存方式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY生物活性4SC-207是一種強(qiáng)效的、口服有效的微管(microtubule)抑制劑。4SC-207通過抑制微管生長來抑制體外和體內(nèi)腫瘤細(xì)胞的增殖，并促進(jìn)有絲分裂延遲/阻滯，隨后誘導(dǎo)細(xì)胞凋亡(apoptosis)或異常分裂。4SC-207可抑制紫杉烷類耐藥異種移植小鼠模型中的腫瘤生長。4SC-207可用于癌癥研究，例如結(jié)腸腺癌和其他惡性腫瘤[1]。體外研究4SC-207(10nM-100μM,24-72h)reducescellviabilityandinducesaG2/MarrestonlyinproliferatingRKOcells[1].4SC-207(10nM-100nM,9h)induces,inadosedependentmanner,aberrantdivisions,followingaprolongedmitosis,ormitoticarrestinHeLawtcells,andaffectsallcellsat100nM[1].4SC-207(0-2μM,0-20min)inhibitstubulinpolymerizationinadose-dependentmannerinaninvitroassayusingpurifiedpig-braintubulin[1].4SC-207(50-100nM)reducesmicrotubulegrowthspeedsinlivingHeLacells[1].4SC-207(72h)exhibitspotentanti-proliferativeagentactiveonabroadrangeoftumorcellswithanaverageGI50of11nM,andisactiveinmulti-drugresistantcelllines,suchasHCT-15andACHN[1].CellViabilityAssay[1]CellLine:RKOcellsConcentration:10nM-100μMIncubationTime:72hResult:Reducedthepercentageofviablecellsfrom100%to20%whenaddedatorabovea1/2 MasterofBioactiveMolecules—您身邊的抑制劑大師www.MedChemEconcentrationof100nM.CellCycleAnalysis[1]CellLine:RKOcellsConcentration:100nMIncubationTime:24hResult:ShowedastrongincreaseinthepercentageofcellsinG2/Mphase(52%comparedto24%ofDMSO-treatedcells).DecreasedtheamountofcellsinG1andSphases(respectively14%and10%comparedto53%and20%incontrolcells).體內(nèi)研究4SC-207(60and120mg/kg,i.g.,3timesweeklyfor3weeks)showsanti-proliferativeactivityalsointhecontextofatumorresistanttoTaxol(HY-B0015)treatmentinanHCT-15xenograftmousemodel[1].AnimalModel:FemaleSCIDmicesubcutaneouslyimplantedwithHCT-15coloncancercells[1]Dosage:60and120mg/kgAdministration:i.g.,3timesweeklyfor3weeksResult:Resultedinareductionintumorgrowth,inadosedependentmanner,withoutevidenceoftoxicitybasedonbodyweightmeasurements.Resultedinsignificanttumorreductionatday12,day14,andday19at120mg/kg.REFERENCESBauschE,etal.Anovelmicrotubuleinhibitor4SC-207withanti-proliferativeactivityintaxane-resistantcells.PLoSOne.2013Nov6;8(11):e79594.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications