Cimpuciclib-tosylate-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemECimpuciclibtosylateCat.No.:HY-112243ACASNo.:2408872-84-2分⼦式:C₃₇H₄₃FN₈O₄S分⼦量:714.85作⽤靶点:CDK作⽤通路:CellCycle/DNADamage储存⽅式:4°C,sealedstorage,awayfrommoisture*Insolvent:-80°C,6months;-20°C,1month(sealed

storage,awayfrommoisture)溶解性数据体外实验DMSO:200mg/mL(279.78mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM1.3989mL6.9945mL13.9889mL5mM0.2798mL1.3989mL2.7978mL10mM0.1399mL0.6994mL1.3989mL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Cimpuciclibtosylate⼀种选择性的CDK4抑制剂(IC50:0.49nM)，具有抗肿瘤活性。IC50&TargetCDK4CDK60.49nM(IC50)9.56nM(IC50)体外研究Cimpuciclib(example63,141.2nM,6days)tosylateinhibitsproliferationofcolo205cells[1].1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemECellProliferationAssay[1]CellLine:Colo205cellsConcentration:0-500nMapproximatelyIncubationTime:6daysResult:InhibitedcellproliferationwithanIC50valueof141.2nM.体内研究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