Biological Activity
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[1].
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[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].
In Vivo
SR-717 (30 mg/kg intraperitoneal once-per-day for 1 week) shows antitumor activities in WT or Stinggt/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 Stinggt/gt mice[1] Dosage: 30 mg/kg Administration: Intraperitoneally; once-per-day for 1 week Result: Maximally inhibited tumor growth.
References & source
[1] Gajewski and Higgs, (2020). Immunotherapy with a sting. Science, DOI: 10.1126/science.abc6622. [2] Chin et al, (2020). Antitumor activity of a systemic STING-activating non-nucleotide cGAMP mimetic. Science, 10.1126/science.abb4255 [3] Pan et al, (202
Published experimental findings depend on the model and assay conditions. They do not guarantee equivalent performance in every application. For laboratory research use only.