Sodium-stibogluconate-Stibogluconate-trisodium-nonahydrate-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemESodiumstibogluconateCat.No.:HY-100595CASNo.:16037-91-5Synonyms:Stibogluconatetrisodiumnonahydrate分⼦式:C₁₂H₃₈Na₃O₂₆Sb₂分⼦量:910.9作⽤靶点:Phosphatase;Parasite;SHP2作⽤通路:MetabolicEnzyme/Protease;Anti-infection;ProteinTyrosineKinase/RTK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H2O:3mg/mL(3.29mM;ultrasonicandwarmingandheatto60°C)DMSO:1mg/mL(1.10mM;Needultrasonicandwarming)MassSolvent1mg5mg10mgConcentration制备储备液1mM1.0978mL5.4891mL10.9782mL5mM---------10mM---------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。BIOLOGICALACTIVITY⽣物活性Sodiumstibogluconate(Stibogluconatetrisodiumnonahydrate)蛋⽩酪氨酸磷酸酶(phosphatase)的有效抑制剂。Sodiumstibogluconate在10，100和100μg/mL时分别抑制99%的SHP-1，SHP-2和PTP1B活性。1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEIC50&TargetPhosphatase[1]体外研究Sodiumstibogluconate(Stibogluconatetrisodiumnonahydrate)inhibits99%ofSHP-1activityat10μg/mL,atherapeuticconcentrationofthedrugforleishmaniasis.SimilardegreesofinhibitionofSHP-2andPTP1Brequired100μg/mLSodiumstibogluconate.TheinhibitionofcellularPTPasesbytheSodiumstibogluconateissuggestedbyitsrapidinductionoftyrosinephosphorylationofcellularproteinsinBaf3cellsanditsaugmentationofIL-3-inducedJanusfamilykinase2/Stat5tyrosinephosphorylationandproliferationofBaf3cells.TheaugmentationoftheoppositeeffectsofGM-CSFandIFN-αonTF-1cellgrowthbySodiumstibogluconateindicateitsbroadactivitiesinthesignalingofvariouscytokines[1].体内研究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.户使⽤本产品发表的科研⽂献•JExpClinCancerRes.2019Feb14;38(1):80.•CellRep.2022Apr12;39(2):110622.•ParasitVectors.2020Oct12;13(1):510.•ParasitVectors.2020Feb21;13(1):94.Seemorecustomervalidationsonwww.MedChemEREFERENCES2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师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