SR-717 is a non-nucleotide STING agonist with EC50s of 2.1 μM and 2.2 μM in ISG-THP1 (WT) and ISG-THP1 cGAS KO (cGAS KO) cell lines, respectively. SR-717 is a stable cyclic guanosine monophosphate-adenosine monophosphate (cGAMP) mimetic. Antitumor activity.In Vitro: 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.
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.In Vivo: SR-717 (30 mg/kg intraperitoneal once-per-day for 1 week) shows antitumor activities in WT or Stinggt/gt mice.
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.