Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEPLK1-IN-13Cat.No.:HY-173212CASNo.:3038489-48-1分?式:C??H??N?O?S分?量:577.74作?靶點:Polo-likeKinase(PLK);c-Myc;Apoptosis作?通路:CellCycle/DNADamage;Apoptosis儲存?式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY?物活性PLK1-IN-13?種選擇性和?服活性的PLK1抑制劑(IC50:0.27nM)。PLK1-IN-13還抑制PLK2(IC50:12.72nM)和PLK3(IC50:4.12nM)。PLK1-IN-13將細胞停滯在G2期，誘導細胞凋亡(apoptosis)并下調增殖相關致癌因c-MYC的轉錄。PLK1-IN-13抑制腫瘤?長，可?于急性髓系??病(AML)的研究[1]。IC50&TargetPLK1PLK2PLK30.27nM(IC50)12.72nM(IC50)4.12nM(IC50)體外研究PLK1-IN-13(CompoundWD6)(72h)hasantiproliferativeactivitiesagainstMDA-MB-231(IC50:9.5nM)andMV4-11cell(IC50:23.3nM),andtheIC50forMCF-7andHCT-116are47.1nMand59.9nMrespectively[1].PLK1-IN-13hasweakinhibitoryeffectsonCYP2C9(IC50:7.39μM),CYP2C19(IC50:14μM),CYP2D6(IC50:13.8μM),andCYP3A4(IC50:17.3μM),indicatingthatPLK1-IN-13mayhavelowerdrug-druginteractions[1].PLK1-IN-13(2.92nM-46.6nM,72h)inducesG2/Mcell-cyclearrestandinducesapoptosisinMV4-11cells[1].PLK1-IN-13(0-1μM,24h)down-regulatesthetranscriptionoftheproliferation-relatedoncogenec-MYCinMV4-11cells[1].ApoptosisAnalysis[1]CellLine:MV4-11cellsConcentration:2.92nM,5.83nM,11.6nM,23.3nM,and46.6nM1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEIncubationTime:72hResult:Increasedthecellapoptosisrate,rangingfrom3.29%to67.7%inaconcentration-dependentmanner.體內研究PLK1-IN-13(CompoundWD6)(20mg/kg,p.o.,onceadayfor19consecutivedays)inhibitsthetumorgrowth(TGI=91.2%)inxenograftmousemodelsofMV4-11[1].PLK1-IN-13(10,20mg/kg,i.g.)showsagoodhalf-life,highplasmaexposure,andmoderatebioavailabilityinSDrats[1].AnimalModel:subcutaneousxenograftmousemodelsofMV4-11,Balb/cnudemice[1]Dosage:20mg/kgAdministration:p.o.,onceadayfor19consecutivedays.Result:Inhibitedthetumorgrowth(TGI=91.2%).Showednosignificantweightlossordeathinmice.REFERENCES[1].HouY,etal.DiscoveryofnoveldihydropteridonederivativesasorallybioavailablePLK1inhibitorswithreducedhERGinhibitoryactivityforacutemyeloidleukemiatreatment.EurJMedChem.2025May5;289:117480.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresear