CDK9-IN-22-DataSheet-生命科学试剂-MCE

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemECDK9-IN-22Cat.No.:HY-151984分⼦式:C₂₈H₂₈FN₅O₂分⼦量:485.55作⽤靶点:CDK作⽤通路:CellCycle/DNADamage储存⽅式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY⽣物活性CDK9-IN-22⼀种有效的CDK9抑制剂，对CDK9和CDK的IC50分别为10.4、876.2nM。CDK9-IN-22诱导细胞凋亡(apoptosis)和细胞周期停滞在G2/M期。CDK9-IN-22降低p-RNAPII(S2)和CDK9蛋⽩的表达。CDK9-IN-22具有抗增殖和抗肿瘤活性[1]。IC50&TargetCDK9/cyclinT1cdk2/cyclinA10.4nM(IC50)876.2nM(IC50)体外研究CDK9-IN-22(compound8d)(0.1,0.5,2.5µM;24,48h)inducesapoptosisandcellcyclearrestsatG2/Mphaseinaconcentration-dependentmannerinPANC-1cells[1].CDK9-IN-22(0.1,0.5,2.5µM;24h)decreasestheexpressionofp-RNAPII(S2)andCDK9proteininPANC-1cells[1].CellProliferationAssay[1]CellLine:A549,H1975,A431,PANC-1,HCT-116,LO2cellsConcentration:0-100µMIncubationTime:72hResult:ShowedantiproliferativeactivitywithIC50sof0.66,0.43,0.10,0.08,0.09,1.43μMforA549,H1975,A431,PANC-1,HCT-116,LO2cells,respectively.ApoptosisAnalysis[1]CellLine:PANC-1cells1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEConcentration:0.1,0.5,2.5µMIncubationTime:48hResult:Inducedapoptosiswiththepercentageoftotalapoptoticcellswas43.6,54.1and65.8%at0.1,0.5and2.5μM,respectively.CellCycleAnalysis[1]CellLine:PANC-1cellsConcentration:0.1,0.5,2.5µMIncubationTime:24hResult:ArrestedthecellcycleattheG2/Mphaseinadose-dependentmanner(21.83%for0.1μM,25.85%for0.5μMand34.26%for2.5μM).WesternBlotAnalysis[1]CellLine:PANC-1cellsConcentration:0.1,0.5,2.5µMIncubationTime:24hResult:Decreasedtheexpressionofp-RNAPII(S2)andCDK9proteininadose-dependentmanner.体内研究CDK9-IN-22(5,10,20mg/kg;i.p.;everyotherdayforfourweeks)inhibitstumorgrowthinxenograftmurinemodel[1].AnimalModel:BALB/cnudemice(PANC-1tumorxenograftmurinemodel)[1]Dosage:5,10,20mg/kgAdministration:I.p.;everyotherdayforfourweeksResult:Inhibitedthetumorgrowthwiththetumorinhibitionrate(TIR)was6.2,32.6and54.2%atthedoseof5,10and20mg/kg,respectively.REFERENCES[1].XuZ,etal.Design,synthesisandanticancerevaluationofselective2,4-disubstitutedpyrimidineCDK9inhibitors.EurJMedChem.2022Dec15;244:114875.McePdfHeight2/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemECaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forr