GSK2837808A-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEGSK2837808ACat.No.:HY-100681CASNo.:1445879-21-9分⼦式:C₃₁H₂₅F₂N₅O₇S分⼦量:649.62作⽤靶点:LactateDehydrogenase作⽤通路:MetabolicEnzyme/Protease储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:50mg/mL(76.97mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM1.5394mL7.6968mL15.3936mL5mM0.3079mL1.5394mL3.0787mL10mM0.1539mL0.7697mL1.5394mL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。-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(3.85mM);Clearsolution1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEBIOLOGICALACTIVITY⽣物活性GSK2837808A有效和选择性的乳酸脱氢酶A(LDHA)抑制剂，对hLDHA和hLDHB的IC50值分别为2.6和43nM。IC50&TargetIC50:2.6nM(hLDHA),43nM(hLDHB)[1]体外研究GSK2837808Arapidlyandprofoundlyinhibitslactateproductionratesinmultiplecancercelllinesincludinghepatocellularandbreastcarcinomas.ThepotencyofGSK2837808Aacross30cancercelllineswithdifferentLDHAandLDHBexpressionlevelsrangesfrom400nMtonoeffect(EC50reportedas30μM).GSK2837808ApotencydoesnotcorrelatewithLDHA,LDHB,orthetotalLDHexpressionlevels.GSK2837808Ainhibitslactateproductioninhypoxiabutathigherconcentrationsthaninnormoxia(EC50=10μM).ItalsoreducesECARwithEC50=10μM.LDHinhibitionbyGSK2837808AaltersmultiplemetabolicpathwaysinSnu398cells[1].体内研究ClearancefollowingIVinfusionofGSK2837808Aat0.25mg/kgisshowntobe69mL/minute/kginrats,whichexceedstheanimalliverbloodflow.OraldosingofGSK2837808Aat50mg/kginratsor100mg/kginmiceresultsinbloodcompoundlevelsatorbelowthedetectionlimitof2.5ng/mL[1].PROTOCOLCellAssay[1]SixtythousandSnu398cellsperwellareplatedin6-welltissuecultureplatesinRPMI-1640mediumsupplementedwith2.5%charcoal-strippedFBS.CellsareallowedtoattachovernightandthenDMSOcontrolortheindicateddosesofLDHAinhibitordissolvedinDMSOareaddeddirectlytothewells.After4to8daysofincubationintheindicatedoxygenconditions,adherentcellsaretrypsinized,counted,andhadtheirviabilityassessedbythetrypan-blueexclusionmethodusingtheVi-CellXRCellViabilityAnalyzer[1].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.AnimalMice:GSK2837808AisadministeredtomaleCDmiceormaleSprague-DawleyratsorallyorbyintravenousAdministration[1](IV)infusionover120minutesintoafemoralvein.ArterialbloodsamplesarecollectedovertimeandGSK2837808Aconcentrationisdeterminedbyliquidchromatography(LC)/MS/MSanalysis[1].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.户使⽤本产品发表的科研⽂献•NatCommun.2020Jul9;11(1):3427.•NatCommun.2020Jun22;11(1):3162.•NatCommun.2019Jun20;10(1):2701.•JExpClinCancerRes.2021Dec10;40(1):390.•CellMolLifeSci.2019Apr;76(8):1579-1593.Seemorecustomervalidationsonwww.MedChemE2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEREFERENCES[1].BilliardJ,etal.Quinoline3-sulfonamidesinhibitlactatedehydrogenaseAandreverseaerobicglycolysisincancercells.CancerMetab.2013Sep6;1(1):19.McePdfHeightCaution:Product