GSK2837808A-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEGSK2837808ACat.No.:HY-100681CASNo.:1445879-21-9分?式:C??H??F?N?O?S分?量:649.62作?靶點:LactateDehydrogenase作?通路:MetabolicEnzyme/Protease儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實驗DMSO:50mg/mL(76.97mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM1.5394mL7.6968mL15.3936mL5mM0.3079mL1.5394mL3.0787mL10mM0.1539mL0.7697mL1.5394mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；?旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲備液的保存?式和期限：-80°C,6months;-20°C,1month。-80°C儲存時，請在6個?內(nèi)使?，-20°C儲存時，請在1個?內(nèi)使?。體內(nèi)實驗請根據(jù)您的實驗動物和給藥?式選擇適當(dāng)?shù)娜芙?案。以下溶解?案都請先按照InVitro?式配制澄的儲備液，再依次添加助溶劑：(為保證實驗結(jié)果的可靠性，澄的儲備液可以根據(jù)儲存條件，適當(dāng)保存；體內(nèi)實驗的?作液，建議您現(xiàn)?現(xiàn)配，當(dāng)天使?；以下溶劑前顯?的百分?指該溶劑在您配制終溶液中的體積占?；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的?式助溶)1.請依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.5mg/mL(3.85mM);Clearsolution1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEBIOLOGICALACTIVITY?物活性GSK2837808A有效和選擇性的乳酸脫氫酶A(LDHA)抑制劑，對hLDHA和hLDHB的IC50值分別為2.6和43nM。IC50&TargetIC50:2.6nM(hLDHA),43nM(hLDHB)[1]體外研究GSK2837808Arapidlyandprofoundlyinhibitslactateproductionratesinmultiplecancercelllinesincludinghepatocellularandbreastcarcinomas.ThepotencyofGSK2837808Aacross30cancercelllineswithdifferentLDHAandLDHBexpressionlevelsrangesfrom400nMtonoeffect(EC50reportedas30μM).GSK2837808ApotencydoesnotcorrelatewithLDHA,LDHB,orthetotalLDHexpressionlevels.GSK2837808Ainhibitslactateproductioninhypoxiabutathigherconcentrationsthaninnormoxia(EC50=10μM).ItalsoreducesECARwithEC50=10μM.LDHinhibitionbyGSK2837808AaltersmultiplemetabolicpathwaysinSnu398cells[1].體內(nèi)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.戶使?本產(chǎn)品發(fā)表的科研?獻(xiàn)?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?邊的抑制劑?師www.MedChemEREFERENCES[1].BilliardJ,etal.Quinoline3-sulfonamidesinhibitlactatedehydrogenaseAandreverseaerobicglycolysisincancercells.CancerMetab.2013Sep6;1(1):19.McePdfHeightCaution:Product