CDK9-IN-22-DataSheet-生命科學(xué)試劑-MCE

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemECDK9-IN-22Cat.No.:HY-151984分?式:C??H??FN?O?分?量:485.55作?靶點(diǎn):CDK作?通路:CellCycle/DNADamage儲(chǔ)存?式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY?物活性CDK9-IN-22?種有效的CDK9抑制劑，對(duì)CDK9和CDK的IC50分別為10.4、876.2nM。CDK9-IN-22誘導(dǎo)細(xì)胞凋亡(apoptosis)和細(xì)胞周期停滯在G2/M期。CDK9-IN-22降低p-RNAPII(S2)和CDK9蛋?的表達(dá)。CDK9-IN-22具有抗增殖和抗腫瘤活性[1]。IC50&TargetCDK9/cyclinT1cdk2/cyclinA10.4nM(IC50)876.2nM(IC50)體外研究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?邊的抑制劑?師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.體內(nèi)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?邊的抑制劑?師www.MedChemECaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forr