Zapnometinib-PD0184264-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEZapnometinibCat.No.:HY-139558CASNo.:303175-44-2Synonyms:PD0184264;ATR-002分⼦式:C₁₃H₇ClF₂INO₂分⼦量:409.55作⽤靶点:MEK;InfluenzaVirus;Bacterial作⽤通路:MAPK/ERKPathway;Anti-infection储存⽅式:4°C,protectfromlight*Insolvent:-80°C,6months;-20°C,1month(protectfrom

light)溶解性数据体外实验DMSO:62.5mg/mL(152.61mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.4417mL12.2085mL24.4170mL5mM0.4883mL2.4417mL4.8834mL10mM0.2442mL1.2209mL2.4417mL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(protectfromlight)。-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:≥2.08mg/mL(5.08mM);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%cornoilSolubility:≥2.08mg/mL(5.08mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性Zapnometinib(PD0184264)CI-1040的活性代谢物，⼀种MEK抑制剂，IC50值为5.7nM。Zapnometinib具有抗流感病毒的抗病毒活性和抗活性。IC50&TargetMEK5.7nM(IC50)体外研究Zapnometinib(0.1nM-1μM)inhibitsMEK,withIC50sof30.96nM,357nM,and15nMincellfreekinaseassay,A549,MDCKcellsandhumanPBMCs[1].Zapnometinib(100μM;4h)inhibitstheIonomycin(PMA/I)-inducedphosphorylationofERK1/2inhumanPBMCs[1].Zapnometinib(1-100μM)reducestheviraltitersoftheIVH1N1pdm09,H3N2[1].WesternBlotAnalysis[1]CellLine:humanPBMCsConcentration:100μMIncubationTime:4hResult:InhibitedtheIonomycin(PMA/I)-increasedpERK1/2.体内研究Zapnometinib(8.4-75mg/kg/day;threetimesadayp.o.)reducesthelungvirustitersandenhancessurvivalofmiceafterlethalH1N1pdm09infection[1].Zapnometinib(150mg/kg)exhibitsAUCvaluesof860.02and1953.68μg•h/mLinmicebyi.v.ororalroute,respectively[1].AnimalModel:FemaleC57BL/6mice(8weeks;21-24g)wereinfectedwithH1N1pdm09[1]Dosage:8.4,25,75mg/kg/day(2.8,8.4,25mg/kg)Administration:P.o.threetimesadayResult:Significantlyreducedthevirustiteratthedoseofeither75mg/kg/dayor25mg/kg/day.REFERENCES[1].LaureM,et,al.AntiviralefficacyagainstinfluenzavirusandpharmacokineticanalysisofanovelMEK-inhibitor,ATR-002,incellcultureandinthemousemodel.AntiviralRes.2020Jun;178:104806.2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE[2].HamzaH,et,al.ImprovedinvitroEfficacyofBaloxavirMarboxilAgainstInfluenzaAVirusInfectionbyCombinationTreatmentWiththeMEKInhibitorATR-002.FrontMicrobiol.2021Feb12;12:611958.[3].BruchhagenC,et,al.MetabolicconversionofCI-1040turnsacellularMEK-inhibitorintoanantibacterialcompound.SciRep.2018Jun14;8(1):9114.McePdfHeightCaution:Producthasnotbeenfullyvalidatedfor