EPZ011989-trifluoroacetate-EPZ-011989-trifluoroacetate-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEEPZ011989trifluoroacetateCat.No.:HY-16986ACASNo.:1598383-41-5Synonyms:EPZ-011989trifluoroacetate分⼦式:C₃₇H₅₂F₃N₅O₆分⼦量:719.83作⽤靶点:HistoneMethyltransferase作⽤通路:Epigenetics储存⽅式:4°C,sealedstorage,awayfrommoisture*Insolvent:-80°C,6months;-20°C,1month(sealed

storage,awayfrommoisture)溶解性数据体外实验DMSO:100mg/mL(138.92mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM1.3892mL6.9461mL13.8922mL5mM0.2778mL1.3892mL2.7784mL10mM0.1389mL0.6946mL1.3892mL请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。储备液的保存⽅式和期限：-80°C,6months;-20°C,1month(sealedstorage,awayfrommoisture)。-80°C储存时，请在6个⽉内使⽤，-20°C储存时，请在1个⽉内使⽤。体内实验请根据您的实验动物和给药⽅式选择适当的溶解⽅案。以下溶解⽅案都请先按照InVitro⽅式配制澄的储备液，再依次添加助溶剂：(为保证实验结果的可靠性，澄的储备液可以根据储存条件，适当保存；体内实验的⼯作液，建议您现⽤现配，当天使⽤；以下溶剂前显⽰的百分⽐指该溶剂在您配制终溶液中的体积占⽐；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的⽅式助溶)1.请依序添加每种溶剂：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.5mg/mL(3.47mM);Clearsolution1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(3.47mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(3.47mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性EPZ-011989trifluoroacetate⼀种有效且代谢稳定的ZesteHomolog2(EZH2)抑制剂，具有⼝服活性。EPZ-011989trifluoroacetate对EZH2具有抑制性抑制作⽤，Ki值<3nM。EPZ-011989trifluoroacetate具有出强⼤的甲标记抑制和抗肿瘤活性。EPZ-011989trifluoroacetate可⽤于多种癌症的研究。IC50&TargetEZH2体外研究EPZ-011989trifluoroacetateinhibitsmutantandwild-typeEZH2withanKivalueof[1].EPZ-011989trifluoroacetatereducescellularH3K27methylationwithanIC50valueof94nM[1].EPZ-011989trifluoroacetate(0-10μM;11days)hasanti-proliferationeffectinWSU-DLCL2cells[1].CellProliferationAssay[1]CellLine:WSU-DLCL2cellsConcentration:0-10μMIncubationTime:11daysResult:Demonstratedanaveragelowestcytotoxicconcentration(LCC)inWSU-DLCL2cellsof208nM.体内研究EPZ-011989trifluoroacetate(oral;30-1000mg/kg;singleorbid;for7daysor21days)canelicitrobustmethylmarkinhibitionandantitumoractivity[1].AnimalModel:SCIDmice[1]Dosage:125,250,500,and1000mg/kgAdministration:Oral;single,twice-daily(BID)for7daysortwice-daily(BID)for21daysResult:ProvidedcoverageovertheLCCfor24h(1000mg/kg),whilethe250and500mg/kgdosesprovidedcoverageoverthisvalueforapproximately8h.Observedcompleteablationofthemethylmarkbytheendofday7.Showedrobusttumorgrowthinhibition,methylmarkreductionandextendedtotalandfreeplasmaexposuretime.AnimalModel:Rat[1]2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEDosage:30,100,and300mg/kgAdministration:Oral,singleResult:dose(mg/kg)routet1/2(h)tmax(h)Cmax(ng/mL)AUCinf(h*ng/mL)timeaboveLCC(h)30p.o.4.722409704100p.o.3.92.7160056008300p.o.3.72.729001000010户使⽤本产品发表的科研⽂献•ProcNatlAcadSciUSA.2019Feb19;116(8):2961-2966.•JImmunotherCancer.2021May;9(5):e001335.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].CampbellJE,etal.EPZ011989,APotent,Orally-AvailableEZH2InhibitorwithRobustinVivoActivity.ACSMedChemLett.2015Mar4;6(5):491-495.McePdfHeightCaution:Producthasnotbeenfu