Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemECITCOCat.No.:HY-103244CASNo.:338404-52-7分?式:C??H??Cl?N?OS分?量:436.74作?靶點(diǎn):Apoptosis作?通路:Apoptosis儲(chǔ)存?式:-20°C,sealedstorage,awayfrommoisture*Insolvent:-80°C,6months;-20°C,1month(sealed

storage,awayfrommoisture)溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:25mg/mL(57.24mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM2.2897mL11.4485mL22.8969mL5mM0.4579mL2.2897mL4.5794mL10mM0.2290mL1.1448mL2.2897mL請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；?旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲(chǔ)備液的保存?式和期限：-80°C,6months;-20°C,1month(sealedstorage,awayfrommoisture)。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)?內(nèi)使?，-20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)?內(nèi)使?。BIOLOGICALACTIVITY?物活性CITCO?種組成型雄甾烷(Constitutiveandrostane)受體激動(dòng)劑，抑制腦腫瘤?細(xì)胞(BTSCs)的?長(zhǎng)和擴(kuò)增。CITCO?種咪唑并噻唑衍?物，其作為?CAR的選擇性激動(dòng)劑起作?。CITCO對(duì)于孕烷X受體(PXR)的EC50為49nM，并且對(duì)其他核受體沒(méi)有活性。IC50&TargetCAR,PXR[1]1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE體外研究CITCO(1-50μM;48?hours)resultsinadose-dependentinhibitionofviablecellcountandproliferationinbothT98GandU87MGgliomaandBTSCs[1].CITCO(2.5,5?μM;48?hours)inducescellcyclearrestdifferentiallyindifferentBTSCsinculture,butnotinnormalastrocytes[1].CITCO(2.5-10?μM;48?hours)inducesapoptosisinBTSCsincultureindosedependently,butnotinnormalastrocytes[1].CITCO(0-25?μM;48?hours)causestheT98GandU87MGgliomaandBTSCsexpressingverylowlevelsofCARproteinthatincreasedsignificantly[1].CellProliferationAssay[1]CellLine:T98G,U87MG,DB29andDB33humangliomacells,astrocytesConcentration:1,2.5,5,10,25,50μMIncubationTime:48?hoursResult:Resultedinadose-dependentinhibitionofviablecellcountandproliferation.CellCycleAnalysis[1]CellLine:TheT98G,U87MG,DB29andDB33gliomacellsConcentration:2.5,5?μMIncubationTime:48?hoursResult:InducedcellcyclearrestdifferentiallyindifferentBTSCsinculture.ApoptosisAnalysis[1]CellLine:TheT98G,U87MG,DB29andDB33gliomacellsConcentration:2.5,5or10?μMIncubationTime:48?hoursResult:IncreasedthelevelsofAnnexinV-positiveapoptoticcellsindosedependently.WesternBlotAnalysis[1]CellLine:T98G,U87MG,DB29andDB33gliomacellsConcentration:0to25?μMIncubationTime:48?hoursResult:TheT98G,U87MGgliomaandBTSCsexpressedverylowlevelsofCARproteinthatincreasedsignificantly.2/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE體內(nèi)研究CITCO(intraperitoneal;ondays22,24,26,30and36)with25?μgresultsasignificantdecreaseintumourgrowth,whichfurtherdecreasestoanundetectablelevelaftertreatmentwith100?μgCITCO[1].AnimalModel:Six-toeight-week-oldmaleathymicnudemice[1]Dosage:25or100?μgAdministration:Intraperitoneal;ondays22,24,26,30and36Result:Decreasedtumourgrowth.REFERENCES[1].ChakrabortyS,etal.ConstitutiveandrostanereceptoragonistCITCOinhibitsgrowthandexpansionofbraintumourstemcells.BrJCancer.2011Feb1;104(3):448-59.McePdfHeightCaution:Producthasnotbeenfullyvalidatedf