Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEPLK1-IN-12Cat.No.:HY-172364分?式:C??H??ClN?O?分?量:558.12作?靶點(diǎn):Polo-likeKinase(PLK)作?通路:CellCycle/DNADamage儲(chǔ)存?式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY?物活性PLK1-IN-12?種?選擇性、具有?服活性的PLK1抑制劑，IC50為20nM。PLK1-IN-12對(duì)PLK1的選擇性?于PLK2(IC50:>10000nM)和PLK3(IC50:3953nM)。PLK1-IN-12在?泛的細(xì)胞系中表現(xiàn)出抗癌效?。PLK1-IN-12能夠?于抗??病研究。IC50&TargetPLK1PLK2PLK320nM(IC50)>10000nM(IC50)3953nM(IC50)體外研究PLK1-IN-12(CompoundB31)(0.508nM-10μM,24h)showsantiproliferativeeffectsinH460(IC50:12nM),A549(IC50:32nM),SW620(IC50:8.2nM),HL-60(IC50:59nM),K562(IC50:0.08nM)andCCRF-CEM(IC50:41nM)celllines[1].PLK1-IN-12(1μM,5min)showsrapidclearanceinhuman,mouseanddoglivermicrosomes(Clint:68.3-210μL/min/mgprotein)[1].PLK1-IN-12(0.1-30μM,24h)hasalowinhibitoryeffectonHEK293Tcellsviability(68%)[1].PLK1-IN-12(0.4-100μM)hasalowinhibitoryeffectonhERGpotassiumchannels(IC50:44.2μM),indicatingalowriskofcardiotoxicity[1].PLK1-IN-12(10μM,5-30min)hasnoinhibitoryeffectonCYP1A2,CYP3A4,CYP2D6,CYP2B6andCYP2C8,andonlyhasweakinhibitoryeffectsonCYP2C9andCYP2C19,indicatingthatitisstableinbothhumanandrathepatocytesandhasalowpossibilityofdruginteractions[1].CellProliferationAssay[1]CellLine:H460、PC-9、A549、SW620、HL-60、K562、CCRF-CEMandKG-1celllinesConcentration:1.00×10-5,3.33×10-6,1.11×10-6,3.7×10-7,1.23×10-7,4.12×10-8,1.37×10-8,1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE4.57×10-9,1.52×10-9,and5.08×10-10mol/LIncubationTime:24hResult:ShowedantiproliferativeeffectsinH460(IC50:12nM),A549(IC50:32nM),SW620(IC50:8.2nM),HL-60(IC50:59nM),K562(IC50:0.08nM)andCCRF-CEM(IC50:41nM)celllines.CellCytotoxicityAssay[1]CellLine:HEK293TcellsConcentration:0.1,0.3,1,3,10,and30μMIncubationTime:24hResult:HadalowinhibitoryeffectoncellviabilityofHEK293Tcells(68%).體內(nèi)研究PLK1-IN-12(CompoundB31)(10/20mg/kg,i.g.,twiceweeklyfor11d)caninhibittumorgrowthinamousesubcutaneousK562celltransplantationtumormodel[1].PLK1-IN-12(500mg/kg,i.g.,oncedailyfor7d)hasnotissuedamageortoxicitytovariousorgansofmice[1].AnimalModel:SubcutaneousK562celltransplantationtumormodel,MaleBALB/cmice(6–8weeksold,weighing18–20g)[1]Dosage:10/20mg/kgAdministration:Intragastric(i.g.),twiceweeklyfor11dResult:Inhibitedtumorgrowth.AnimalModel:Acutetoxicitytest[1]Dosage:500mg/kgAdministration:Intragastric(i.g.),oncedailyfor7dResult:Comparedwiththemiceinthepositivecontrolgroup,therewasnosignificantchangeinbodyweight,andnoobviousdamagetotheheart,kidney,lung,liverandspleen.REFERENCES[1].NieJ,etal.Structure-BasedDiscoveryofaHighlySelective,OralPolo-LikeKinase1InhibitorwithPotentAntileukemicActivity.JMedChem.2025Feb27;68(4):4477-4497.2/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEMcePdfHeightCaution:Producthasnotbeenfullyvalid