Hotline:400-820-3792Inhibitors ? ScreeningLibraries ? Proteinswww.MedChemESTF-1084Cat.No.:HY-141831CASNo.:2298390-71-1分子式:C??H??N?O?P分子量:381.36作用靶點:Phosphodiesterase(PDE)作用通路:MetabolicEnzyme/Protease儲存方式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY生物活性STF-1084是一種特異性的細胞不可滲透的ENPP1競爭性抑制劑(Ki=33nM)。STF-1084通過阻止其被ENPP1降解來提高細胞外cGAMP濃度，提高免疫浸潤。STF-1084與電離輻射(IR)和cGAMP協(xié)同作用，延緩腫瘤進展。STF-1084可用于研究免疫原性低的癌癥[1]。體外研究STF-1084(0.1-106nM)inhibitsextracellularcGAMPdegradation(IC50=340nM),butdoesnotaffectintracellularcGAMPinhumanENPP1transfectedinto293TcGASENPP1?/?cells[1].STF-1084(10μM)inducesIFNB1expressioninCD14+humanENPP1transfectedinto293TcGASENPP1?/?cells[1].STF-1084(50μM,48h)increasesextracellularcGAMPin4T1-luccells,E0771cells,MC38cells,MDA-MB-231cells,MCF-7cellsandNMuMGcellsviaIRstimulation[1].STF-1084(1-106nM)haslowactivitytowardstheectonucleotidasesalkalinephosphatase(Ki,app>100μM)andENPP2(Ki,app=5.5μM)[1].STF-1084(0.1-106nM,16h)isnon-toxictoprimaryhumanPBMCs[1].STF-1084(50μM,16h)hasnoeffectoncytokineproductionwhencGAMPwaselectroporatedintoprimaryhumanPBMCs[1].STF-1084showshighstability(t1/2;159min)inbothhumanandmouselivermicrosomes[1].體內(nèi)研究STF-1084(100μLof1mM,intratumoralinjections,once,onday0,2,4,and7afterIR)increasesexpressionoftumor-associatedCD11c+population,delaystumorprogressionsynergizedwithIRandcGAMPinWTBALB/cJmicebearing4T1-luccells[1].AnimalModel: WTBALB/cJmice(Five-tonine-week-oldfemalemice)bearing4T1-luccells((1x106)1/2 MasterofBioactiveMolecules—您身邊的抑制劑大師www.MedChemEwereorthotopicallyinjectedonday0)[1]Dosage:100μLof1mMAdministration:intratumoralinjections,once,onday0,2,4,and7afterIRResult:Increasedexpressionoftumor-associatedCD11c+population,delayedtumorprogressionsynergizedwithIRandcGAMP.REFERENCESCarozzaJA,etal.ExtracellularcGAMPisacancercell-producedimmunotransmitterinvolvedinradiation-inducedanti-cancerimmunity.NatCancer.2020Feb;1(2):184-196.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseo