Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEBSP16Cat.No.:HY-151264CASNo.:2727249-47-8分?式:C??H??O?Se分?量:369.27作?靶點:STING作?通路:Immunology/Inflammation儲存?式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY?物活性BSP16?種有效的?擾素因激動劑(STING)激動劑，具有?服活性。BSP16可以選擇性地刺激STING通路。BSP16可?于癌癥研究。IC50&TargetIC50forSTING:9.24μM(ISG-THP1cells);5.71μM(ISGRAW264.7cells)[1]體外研究BSP16(0.1-100μM)canselectivelystimulatetheSTINGpathwayinISG-THP1andISGRAW264.7cellswithEC50valuesof9.24and5.71μM,respectively[1].BSP16(10,25,50μM;1,3,6h)stronglyactivatesSTINGsignalinginhumanandmousecellsandbindsSTINGasahomodimer[1].BSP16exhibitsapromisingabsorption,distribution,metabolism,excretionandtoxicity[1].RT-PCR[1]CellLine:ISG-THP1cellsConcentration:10,25,50μMIncubationTime:1,3,6hResult:RobustlyinducedmRNAexpressionoftargetgenesIFNβ,CXCL10,andIL6inresponsetoSTINGactivation,inatimeandconcentration-dependentmannerinISGTHP1cells.WesternBlotAnalysis[1]CellLine:ISG-THP1cells1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEConcentration:10,25,50μMIncubationTime:1,3,6hResult:RapidlyincreasedthephosphorylationofTBK1andIRF3inaconcentration-dependentmanner.體內(nèi)研究BSP16(po,50mg/kg;iv,5mg/kg)haswellleratedandexcellentpharmacokineticprofile[1].BSP16(oral,15and30mg/kg,q3d;oral,20mg/kg,q5d)inducestumorregressionanddurableantitumorimmunity[1].AnimalModel:MC38(coloncarcinoma)syngeneictumormodel[1]Dosage:15,30mg/kgAdministration:oral,q3dResult:Exhibitedtoleratedandexcellentantitumorefficacy,experiencedcompletetumorregression(CR)afterday21.ResultedinrobustinductionofIFNBandIL6(30mg/kg).AnimalModel:CT26(coloncarcinoma)tumormodel[1]Dosage:20mg/kgAdministration:oral,q5dResult:Exhibitedtoleratedandinducedtumorregressioninalltreatedmicewithin30days.LedtoasubstantialelevationofIFNBintheplasmainCT26bearingmice.AnimalModel:Rats[1]Dosage:5mg/kg,50mg/kgAdministration:oralandi.vResult:compd.adm.Cmax(μg/mL)AUG0-∞(h*μg/mL)t1/2(h)Vss(L/kg)CL(L/h/kg)F(%)BSP16po(50mg/kg)58.2315.91.600.380.16107iv(5mg/kg)29.41.040.260.17REFERENCES[1].XiFeng,etal.DiscoveryofSelenium-ContainingSTINGAgonistsasOrallyAvailableAntitumorAgents.JMedChem.2022Sep7.McePdfHeight2/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemECaution:Producthasnotbeenfullyvalidatedformedicalapplications.F