Hotline:400-820-3792Inhibitors?Agonists?ScreeningLibrarieswww.MedChemESR-717Cat.No.:HY-131454CASNo.:2375421-09-1分?式:C??H?F?LiN?O?分?量:351.19作?靶點(diǎn):STING作?通路:Immunology/Inflammation儲(chǔ)存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:14.29mg/mL(40.69mM;Needultrasonic)H2O:<0.1mg/mL(insoluble)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM2.8475mL14.2373mL28.4746mL5mM0.5695mL2.8475mL5.6949mL10mM0.2847mL1.4237mL2.8475mL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，并請注意儲(chǔ)備液的保存?式和期限。體內(nèi)實(shí)驗(yàn)請根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥?式選擇適當(dāng)?shù)娜芙?案，配制前請先配制澄的儲(chǔ)備液，再依次添加助溶劑(為保證實(shí)驗(yàn)結(jié)果的可靠性，體內(nèi)實(shí)驗(yàn)的?作液，建議您現(xiàn)?現(xiàn)配，當(dāng)天使?；澄的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；以下溶劑前的百分?指該溶劑在您配制終溶液中的體積占?)：1.請依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:1.43mg/mL(4.07mM);Suspendedsolution;Needultrasonic2.請依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:1.43mg/mL(4.07mM);Suspendedsolution;Needultrasonic3.請依序添加每種溶劑：10%DMSO>>90%cornoil1/2MasterofSmallMolecules—您?邊的抑制劑?師www.MedChemESolubility:≥1.43mg/mL(4.07mM);ClearsolutionBIOLOGICALACTIVITY?物活性SR-717?種?核苷類STING激動(dòng)劑，在ISG-THP1(WT)和ISG-THP1cGASKO(cGASKO)細(xì)胞中的EC50分別為2.1μM和2.2μM。SR-717?種穩(wěn)定的環(huán)鳥苷單磷酸腺苷單磷酸(cGAMP)類似物。具有抗腫瘤活性[1]。體外研究SR-717activatesSTINGbyinducingthesameclosedconformation,whichtherebyprovidesanavenuetoexplorethisclassofsystemicSTINGagonistindiversecontexts,includingantitumorimmunity[1].SR-717(3.8μM)inducestheexpressionofPD-L1inTHP1cellsandinprimaryhumanperipheralbloodmononuclearcellsinaSTING-dependentmanner[1].體內(nèi)研究SR-717(30mg/kgintraperitonealonce-per-dayfor1week)showsantitumoractivitiesinWTorStinggt/gtmice[1].SR-717(30mg/kgintraperitoneallyfor7days)displaysantitumoractivity;promotstheactivationofCD8+T,naturalkiller,anddendriticcellsinrelevanttissues;andfacilitatesantigencross-priming[1].AnimalModel:WTorStinggt/gtmice[1]Dosage:30mg/kgAdministration:Intraperitoneally;once-per-dayfor1weekResult:Maximallyinhibitedtumorgrowth.REFERENCES[1].EmilyNChin,etal.AntitumoractivityofasystemicSTING-activatingnon-nucleotidecGAMPmimetic.Science.2020Aug21;369(6506):993-999.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearch