PLK1-BRD4-IN-5-DataSheet-生命科学试剂-MCE

Hotline:400-820-3792Inhibitors • ScreeningLibraries • Proteinswww.MedChemEPLK1/BRD4-IN-5Cat.No.:HY-158031分子式: C₃₁H₄₄N₈O₃分子量: 576.73作用靶点: Apoptosis;Polo-likeKinase(PLK);EpigeneticReaderDomain作用通路: Apoptosis;CellCycle/DNADamage;Epigenetics储存方式: PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY生物活性PLK1/BRD4-IN-5(CompoundSC10)是一种具有口服活性的的PLK1和BRD4抑制剂，对PLK1和BRD4的IC50值分别为0.3 nM和60.8 nM。PLK1/BRD4-IN-5可诱导MV4-11细胞阻滞(cellcyclearrest)于S期并呈剂量依赖性地诱导凋亡(apoptosis)。PLK1/BRD4-IN-5可用于癌症研究[1]。IC50&TargetPLK1BRD40.3nM(IC50)60.8nM(IC50)体外研究PLK1/BRD4-IN-5(CompoundSC10)showssignificantanti-proliferationactivityagainstallthreetumorcelllines(MDA-MB-231IC50 = 17.3 nM,MDA-MB-361IC50 = 8.4 nM,MV4-11IC50 = 5.4 nM)[1].ApoptosisAnalysis[1]CellLine:MV4-11cellsConcentration:0.675nM,1.35nM,2.7nM,5.4nMand10.8nMIncubationTime:72hResult:Exhibitedanincreasingrateofapoptosisrangingfrom6.65to58.35%inaconcentration-dependentmanner.体内研究PharmacokineticparametersofcompoundsinSprague-DawleyRats[1]RouteDose(mg/kg)T1/2(h)Tmax(h)Cmax(ng/mL)AUC0-t(ng•h/mL)Cl(mL•min/kg)MRT0-t(h)Vdss(L/kg)F(%)i.g.103.752.00108657/5.26/21.4i.v.14.9//30353.64.3916.4/1/2 MasterofBioactiveMolecules—您身边的抑制剂大师www.MedChemEREFERENCESLiuJ,etal.DiscoveryandoptimizationofdihydropteridonederivativesasnovelPLK1andBRD4dualinhibitorforthetreatmentofcancer.BioorgMedChem.2024;101:117McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly.Tel:400-820-3792;021-58955