ADU-S100-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•Agonists•ScreeningLibrarieswww.MedChemEADU-S100Cat.No.:HY-12885CASNo.:1638241-89-0分⼦式:C₂₀H₂₄N₁₀O₁₀P₂S₂分⼦量:690.54作⽤靶点:STING作⽤通路:Immunology/Inflammation储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1monthBIOLOGICALACTIVITY⽣物活性ADU-S100(MIW815)⼲扰素因刺激物的激活剂(STING)，具有有效的抗肿瘤和免疫活性[1]。IC50&TargetSTING[1]体外研究ADU-S100showsenhancedtypeIIFNproductionoverCDAinTHP-1humanmonocytes.Incontrast,thedithio,mixed-linkagecyclicdinucleotide(CDN)derivatives(MLRR-CDA,MLRR-S2CDG,andMLRR-S2cGAMP)potentlyactivateallfivehSTINGalleles,includingtherefractoryhSTINGREFandhSTINGQalleles.ADU-S100inducesthehighestexpressionofIFN-βandthepro-inflammatorycytokinesTNF-α,IL-6,andMCP-1onamolarequivalentbasis,ascomparedtoendogenousMLcGAMPandtheTLR3agonistpolyI:C.ADU-S100isalsofoundtoinduceaggregationofSTINGandinducephosphorylationofTBK1andIRF3inmousebonemarrowmacrophage(BMM).ADU-S100inducessignificantlyhigherlevelsofIFN-αwhencomparedtoMLcGAMP[1].体内研究ADU-S100showshigheranti-tumorcontrolthantheendogenousMLcGAMP.AdoseresponseoftheADU-S100compoundisperformedinB16tumor-bearingmice,whichidentifiesanoptimalantitumordoselevelthatalsoelicitesmaximumtumorantigen-specificCD8+Tcellresponses,andimproveslong-termsurvivalto50%[1].PROTOCOLCellAssay[1]CryopreservedhPBMCsarethawedand1×106cellsperwellareplatedina96wellplateinRPMImedia.Cellsarestimulatedwith10μMADU-S100orMLcGAMPfor6hoursandsupernatantsareharvested.1/3www.MedChemEwww.MedChemESupernatantsarediluted1:2andassayedforIFN-αproteinusingCytometricBeadArray(CBA)HumanFlexSet.DataiscollectedusingaFACSVersecytometerandanalyzedbyFCAPArraySoftware[1].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.AnimalMice[1]Administration[1]WTC57BL/6miceareinoculatedwith5×104B16.F10cellsintheleftflank(n=8).Whentumorvolumesare100mm3micereceivethreeITdosesofeitherMLRR-S2CDG(25μg),ADU-S100(50μg),orHBSSascontrol.WTC57BL/6miceareinoculatedwith5×104B16.F10cellsintheleftflank(n=5).Whentumorvolumesare100mm3theyreceivedthreeITdosesofADU-S100at5,25,50or100μgorHBSSascontrol.WTC57BL/6miceareinoculatedwith5×104B16.F10cellsintheleftflank(n=8).Whentumorvolumesare100mm3theyreceivethreeITdosesof100μgADU-S100orHBSSascontrol.Treatmentsareadministeredondays13,17and20andtumormeasurementsaretakentwiceweekly.ResultsareshownaspercentsurvivalbyLog-rank(Mantel-Cox)test(AandC)[1].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.户使⽤本产品发表的科研⽂献•CancerCell.2020Mar16;37(3):289-307.e9.•Biomaterials.2018May;163:67-75.•JImmunotherCancer.2019Sep18;7(1):252.•EnvironInt.2020Oct;143:105949.•ActaCrystallogrDStructBiol.2020Sep1;76(Pt9):889-898.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].CorralesL,etal.DirectActivationofSTINGintheTumorMicroenvironmentLeadstoPotentandSystemicTumorRegressionandImmunity.CellRep.2015May19;11(7):1018-30.McePdfHeight2/3www.MedChemEwww.MedChemE关注MCE中国公众号，

获取前沿资讯、最新活动和

实⽤科研⼯具MedChemExpress(MCE)只为有资质的科研机构、医药企业基于科学研究或药证申报的⽤途提供医药研发服务，