CITCO-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemECITCOCat.No.:HY-103244CASNo.:338404-52-7分⼦式:C₁₉H₁₂Cl₃N₃OS分⼦量:436.74作⽤靶点:Apoptosis作⽤通路:Apoptosis储存⽅式:-20°C,sealedstorage,awayfrommoisture*Insolvent:-80°C,6months;-20°C,1month(sealed

storage,awayfrommoisture)溶解性数据体外实验DMSO:25mg/mL(57.24mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.2897mL11.4485mL22.8969mL5mM0.4579mL2.2897mL4.5794mL10mM0.2290mL1.1448mL2.2897mL请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。储备液的保存⽅式和期限：-80°C,6months;-20°C,1month(sealedstorage,awayfrommoisture)。-80°C储存时，请在6个⽉内使⽤，-20°C储存时，请在1个⽉内使⽤。BIOLOGICALACTIVITY⽣物活性CITCO⼀种组成型雄甾烷(Constitutiveandrostane)受体激动剂，抑制脑肿瘤⼲细胞(BTSCs)的⽣长和扩增。CITCO⼀种咪唑并噻唑衍⽣物，其作为⼈CAR的选择性激动剂起作⽤。CITCO对于孕烷X受体(PXR)的EC50为49nM，并且对其他核受体没有活性。IC50&TargetCAR,PXR[1]1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE体外研究CITCO(1-50μM;48ꢀhours)resultsinadose-dependentinhibitionofviablecellcountandproliferationinbothT98GandU87MGgliomaandBTSCs[1].CITCO(2.5,5ꢀμM;48ꢀhours)inducescellcyclearrestdifferentiallyindifferentBTSCsinculture,butnotinnormalastrocytes[1].CITCO(2.5-10ꢀμM;48ꢀhours)inducesapoptosisinBTSCsincultureindosedependently,butnotinnormalastrocytes[1].CITCO(0-25ꢀμM;48ꢀhours)causestheT98GandU87MGgliomaandBTSCsexpressingverylowlevelsofCARproteinthatincreasedsignificantly[1].CellProliferationAssay[1]CellLine:T98G,U87MG,DB29andDB33humangliomacells,astrocytesConcentration:1,2.5,5,10,25,50μMIncubationTime:48ꢀhoursResult:Resultedinadose-dependentinhibitionofviablecellcountandproliferation.CellCycleAnalysis[1]CellLine:TheT98G,U87MG,DB29andDB33gliomacellsConcentration:2.5,5ꢀμMIncubationTime:48ꢀhoursResult:InducedcellcyclearrestdifferentiallyindifferentBTSCsinculture.ApoptosisAnalysis[1]CellLine:TheT98G,U87MG,DB29andDB33gliomacellsConcentration:2.5,5or10ꢀμMIncubationTime:48ꢀhoursResult:IncreasedthelevelsofAnnexinV-positiveapoptoticcellsindosedependently.WesternBlotAnalysis[1]CellLine:T98G,U87MG,DB29andDB33gliomacellsConcentration:0to25ꢀμMIncubationTime:48ꢀhoursResult:TheT98G,U87MGgliomaandBTSCsexpressedverylowlevelsofCARproteinthatincreasedsignificantly.2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE体内研究CITCO(intraperitoneal;ondays22,24,26,30and36)with25ꢀμgresultsasignificantdecreaseintumourgrowth,whichfurtherdecreasestoanundetectablelevelaftertreatmentwith100ꢀμgCITCO[1].AnimalModel:Six-toeight-week-oldmaleathymicnudemice[1]Dosage:25or100ꢀμgAdministration:Intraperitoneal;ondays22,24,26,30and36Result:Decreasedtumourgrowth.REFERENCES[1].ChakrabortyS,etal.ConstitutiveandrostanereceptoragonistCITCOinhibitsgrowthandexpansionofbraintumourstemcells.BrJCancer.2011Feb1;104(3):448-59.McePdfHeightCaution:Producthasnotbeenfullyvalidatedf