Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemECimpuciclibtosylateCat.No.:HY-112243ACASNo.:2408872-84-2分?式:C??H??FN?O?S分?量:714.85作?靶點:CDK作?通路:CellCycle/DNADamage儲存?式:4°C,sealedstorage,awayfrommoisture*Insolvent:-80°C,6months;-20°C,1month(sealed

storage,awayfrommoisture)溶解性數(shù)據(jù)體外實驗DMSO:200mg/mL(279.78mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM1.3989mL6.9945mL13.9889mL5mM0.2798mL1.3989mL2.7978mL10mM0.1399mL0.6994mL1.3989mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；?旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲備液的保存?式和期限：-80°C,6months;-20°C,1month(sealedstorage,awayfrommoisture)。-80°C儲存時，請在6個?內(nèi)使?，-20°C儲存時，請在1個?內(nèi)使?。BIOLOGICALACTIVITY?物活性Cimpuciclibtosylate?種選擇性的CDK4抑制劑(IC50:0.49nM)，具有抗腫瘤活性。IC50&TargetCDK4CDK60.49nM(IC50)9.56nM(IC50)體外研究Cimpuciclib(example63,141.2nM,6days)tosylateinhibitsproliferationofcolo205cells[1].1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemECellProliferationAssay[1]CellLine:Colo205cellsConcentration:0-500nMapproximatelyIncubationTime:6daysResult:InhibitedcellproliferationwithanIC50valueof141.2nM.體內(nèi)研究Cimpuciclib(example63,50mg/kg,oralgavage,twiceaweek)tosylateinhibitstumorgrowthincolo205tumor-bearingmice[1].Cimpuciclib(5mg/kgforrats,50mg/kgforcolo205tumor-bearingmice,oraladministration)tosylateshowsslowmetabolicrateandmaintainshighconcentrationintheplasma[1].AnimalModel:Colo205tumor-bearingmice[1]Dosage:50mg/kg,twiceaweekAdministration:OralgavageResult:Inhibitedtumorgrowthby93.63%AnimalModel:Rats,colo205tumor-bearingmice[1]Dosage:5mg/kgforrats,50mg/kgforcolo205tumor-bearingmice.Administration:OraladministrationResult:PharmacokineticprofileofCimpuciclib(example63).doseCmax(ng/mL)Tmax(h)AUC0-24(ng/mL?h)t1/2(h)5mg/kg(rats)559.7654142.450mg/kg(mice)7960113678214.8REFERENCES[1].LiuShiqiang,etal.Preparationofbenzimidazolecompoundaskinaseinhibitor.PatentWO2018045956.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly.Te