PROTAC-CDK12-13-Degrader-1-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEPROTACCDK12/13Degrader-1Cat.No.:HY-151110分⼦式:C₄₅H₄₆N₁₀O₆分⼦量:822.91作⽤靶点:CDK作⽤通路:CellCycle/DNADamage储存⽅式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY⽣物活性PROTACCDK12/13Degrader-1(7f)⼀种⾼效选择性的细胞周期蛋⽩依赖性激酶CDK12/CDK13双重降解剂，其DC50值分别2.2nM和2.1nM。PROTACCDK12/13Degrader-1具有抗增殖活性，可⽤于乳腺癌的研究。IC50&TargetCDK12CDK132.2nM(DC50)2.1nM(DC50)体外研究PROTACCDK12/13Degrader-1(7f)(0.02-10μM,150h)significantlyinhibitstheproliferationofMFM223andMDA-MB-231cellsinadose-dependentmanner[1].PROTACCDK12/13Degrader-1(7f)(500nM,4h)cansignificantlydegradeCDK12andCDK13ofMFM223andMDA-MB-231cellsinadose-dependentmanner[1].Immunofluorescence[1]CellLine:MDA-MB-231celllinesConcentration:1.0μMIncubationTime:15hoursResult:Showed88%degradationforCDK12and74%forCDK13.ActedonCDK12withtheDC50valueof2.2nM,andactedonCDK13withtheDC50valueof2.1nM.体内研究ThepharmacokineticparametersofPROTACCDK12/13Degrader-1(7f)inrats[1].1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEParametersoral(20mg/kg)iv(10mg/kg)ip(20mg/kg)iv(2.5mg/kg)t1/2(h)-5.2810.855.8Tmax(h)5.330.082.170.08Cmax(ng/mL)7.7319892.424.791498.5Cmax(ng/mL)7.7319892.424.791498.5AUC0-t(h*ng/mL)21.837193.3284.8383.9AUC0-∞(h*ng/mL)-7242.7318.5391.55CL(mL/h/kg)-1406.5-6495.4F(%)0.15-10.63-REFERENCES[1].JianzhangYang,etal.DiscoveryofaHighlyPotentandSelectiveDualPROTACDegraderofCDK12andCDK13.JMedChem.2022Aug8.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly.Tel:400-820-3792;021-