Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemESodiumstibogluconateCat.No.:HY-100595CASNo.:16037-91-5Synonyms:Stibogluconatetrisodiumnonahydrate分?式:C??H??Na?O??Sb?分?量:910.9作?靶點(diǎn):Phosphatase;Parasite;SHP2作?通路:MetabolicEnzyme/Protease;Anti-infection;ProteinTyrosineKinase/RTK儲(chǔ)存?式:4°C,sealedstorage,awayfrommoisture*Insolvent:-80°C,6months;-20°C,1month(sealed

storage,awayfrommoisture)溶解性數(shù)據(jù)體外實(shí)驗(yàn)H2O:3mg/mL(3.29mM;ultrasonicandwarmingandheatto60°C)DMSO:1mg/mL(1.10mM;Needultrasonicandwarming)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM1.0978mL5.4891mL10.9782mL5mM---------10mM---------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(chǔ)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(chǔ)備液的保存?式和期限：-80°C,6months;-20°C,1month(sealedstorage,awayfrommoisture)。-80°C儲(chǔ)存時(shí)，請?jiān)?個(gè)?內(nèi)使?，-20°C儲(chǔ)存時(shí)，請?jiān)?個(gè)?內(nèi)使?。BIOLOGICALACTIVITY?物活性Sodiumstibogluconate(Stibogluconatetrisodiumnonahydrate)蛋?酪氨酸磷酸酶(phosphatase)的有效抑制劑。Sodiumstibogluconate在10，100和100μg/mL時(shí)分別抑制99%的SHP-1，SHP-2和PTP1B活性。1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEIC50&TargetPhosphatase[1]體外研究Sodiumstibogluconate(Stibogluconatetrisodiumnonahydrate)inhibits99%ofSHP-1activityat10μg/mL,atherapeuticconcentrationofthedrugforleishmaniasis.SimilardegreesofinhibitionofSHP-2andPTP1Brequired100μg/mLSodiumstibogluconate.TheinhibitionofcellularPTPasesbytheSodiumstibogluconateissuggestedbyitsrapidinductionoftyrosinephosphorylationofcellularproteinsinBaf3cellsanditsaugmentationofIL-3-inducedJanusfamilykinase2/Stat5tyrosinephosphorylationandproliferationofBaf3cells.TheaugmentationoftheoppositeeffectsofGM-CSFandIFN-αonTF-1cellgrowthbySodiumstibogluconateindicateitsbroadactivitiesinthesignalingofvariouscytokines[1].體內(nèi)研究Sodiumstibogluconate(Stibogluconatetrisodiumnonahydrate)induces61%growthinhibitionofRencatumorsinBALB/cmicecoincidentwithanincrease(2-fold)intumor-infiltratingmacrophages.AcombinationofSodiumstibogluconateandIL-2ismoreeffectiveininhibitingtumorgrowth(91%)andinducingtumor-infiltrating(4-fold),whereasIL-2alonehaslittleeffect[2].PROTOCOLCellAssay[1]HumanmyeloidcelllineTF-1ismaintainedinRPMI1640supplementedwith10%FCSand40ng/mLrecombinanthumanGM-CSF.Forcellproliferationassays,cellsarewashedin10%FCSmediumtwice,resuspendedin10%FCSmedium,incubatedat37°Cfor16h,andthenculturedat37°Cin10%FCSmediumcontainingvariousamountsofcytokines,sodiumstibogluconate,orpotassiumantimonyltartratefor3-6days.ThecellnumbersinproliferationassaysaredeterminedbyanMTTassayorbymicroscopiccellcounting[1].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.AnimalBALB/candathymicnudeBALB/cmiceareinoculated(s.c.)attheflankswithRencacells(106cells/site).Administration[2]Fourdaysafterinoculation,themicearesubjectedtonotreatment(control)ortreatmentwithIL-2(105IU/dayfor5daysi.p.),Stibogluconatesodium(12mg/dayi.m.athipregions),orthecombinationofthetwoagentsfor2wk.Tumorvolumeismeasuredduringthestudyperiodandcalculatedusingtheformulaforaprolatespheroid[2].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.戶使?本產(chǎn)品發(fā)表的科研?獻(xiàn)?JExpClinCancerRes.2019Feb14;38(1):80.?CellRep.2022Apr12;39(2):110622.?ParasitVectors.2020Oct12;13(1):510.?ParasitVectors.2020Feb21;13(1):94.Seemorecustomervalidationsonwww.MedChemEREFERENCES2/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE[1].PathakMK,etal.Sodiumstibogluconateisapotentinhibitorofproteintyrosinephosphatasesandaugmentscytokineresponsesinhemopoieticcelllines.JImmunol.2001Sep15;167(6):3391-7.[2].FanKetal.SodiumStibogluconateInteractswithIL-2inAnti-RencaTumorActionviaaTCell-DependentMechanisminConnectionwithInductionofTumor-InfiltratingMacrophages.JImmunol.2005Nov15;175(10):7003-8.Mce