SR-717 free acid is a stable cGAMP mimetic and a non-nucleotide STING agonist. It exhibits antitumor activity with EC50 values of 2.1 μM and 2.2 μM in ISG-THP1 (WT) and ISG-THP1 cGAS KO (cGAS KO) cell lines, respectively.

SR-717 activates STING by inducing the same closed conformation, which thereby provides an avenue to explore this class of systemic STING agonist in diverse contexts, including antitumor immunity[1]. SR-717 (3.8 μM) induces the expression of PD-L1 in THP1 cells and in primary human peripheral blood mononuclear cells in a STING-dependent manner[1].

SR-717 (30 mg/kg intraperitoneal once-per-day for 1 week) shows antitumor activities in WT or Sting gt/gt mice[1]. SR-717 (30 mg/kg intraperitoneally for 7 days) displays antitumor activity; promots the activation of CD8 + T, natural killer, and dendritic cells in relevant tissues; and facilitates antigen cross-priming[1]. Animal Model: WT or Sting gt/gt mice[1]Dosage: 30 mg/kg Administration: Intraperitoneally; once-per-day for 1 week Result: Maximally inhibited tumor growth.