4SC-207-生命科学试剂-MCE

Hotline:400-820-3792Inhibitors • ScreeningLibraries • Proteinswww.MedChemE4SC-207Cat.No.:HY-111251CASNo.:871015-11-1分子式:C₁₉H₁₈N₄O₃S分子量:382.44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4SC-207是一种强效的、口服有效的微管(microtubule)抑制剂。4SC-207通过抑制微管生长来抑制体外和体内肿瘤细胞的增殖，并促进有丝分裂延迟/阻滞，随后诱导细胞凋亡(apoptosis)或异常分裂。4SC-207可抑制紫杉烷类耐药异种移植小鼠模型中的肿瘤生长。4SC-207可用于癌症研究，例如结肠腺癌和其他恶性肿瘤[1]。体外研究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—您身边的抑制剂大师www.MedChemEconcentrationof100nM.CellCycleAnalysis[1]CellLine:RKOcellsConcentration:100nMIncubationTime:24hResult:ShowedastrongincreaseinthepercentageofcellsinG2/Mphase(52%comparedto24%ofDMSO-treatedcells).DecreasedtheamountofcellsinG1andSphases(respectively14%and10%comparedto53%and20%incontrolcells).体内研究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