STF-1084 

STF-1084 is a specific, cell-impermeable, competitive inhibitor of ENPP1 (K_i = 33 nM). STF-1084 increases extracellular cGAMP concentrations by preventing its degradation by ENPP1, thereby enhancing immune infiltration. STF-1084 acts synergistically with ionizing radiation (IR) and cGAMP to delay tumor progression. STF-1084 can be used to study cancers with low immunogenicity^[1].

STF-1084 (0.1-10⁶ nM) inhibits extracellular cGAMP degradation (IC₅₀ = 340 nM), but does not affect intracellular cGAMP in human ENPP1 transfected into 293T cGAS ENPP1^−/− cells^[1].

STF-1084 (10 μM) induces IFNB1 expression in CD14⁺ human ENPP1 transfected into 293T cGAS ENPP1^−/− cells^[1].

STF-1084 (50 μM, 48 h) increases extracellular cGAMP in 4T1-luc cells, E0771 cells, MC38 cells, MDA-MB-231 cells, MCF-7 cells and NMuMG cells via IR stimulation ^[1].

STF-1084 (1-10⁶ nM) has low activity towards the ectonucleotidases alkaline phosphatase (K_i,app > 100 μM) and ENPP2 (K_i,app = 5.5 μM)^[1].

STF-1084 (0.1-10⁶ nM, 16 h) is non-toxic to primary human PBMCs^[1].

STF-1084 (50 μM, 16 h) has no effect on cytokine production when cGAMP was electroporated into primary human PBMCs^[1].

STF-1084 shows high stability (t_1/2; 159 min) in both human and mouse liver microsomes^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

STF-1084 (100 μL of 1 mM, intratumoral injections, once, on day 0, 2, 4, and 7 after IR) increases expression of tumor-associated CD11c⁺ population, delays tumor progression synergized with IR and cGAMP in WT BALB/cJ mice bearing 4T1-luc cells^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

381.36

C₁₇H₂₄N₃O₅P

2298390-71-1

OP(O)(CCC1CCN(C2=C3C=C(OC)C(OC)=CC3=NC=N2)CC1)=O

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Carozza JA, et al. Extracellular cGAMP is a cancer cell-produced immunotransmitter involved in radiation-induced anti-cancer immunity. Nat Cancer. 2020 Feb;1(2):184-196.