SR-717 (2375421-09-1) is a cell permeable and exceptionally selective STING agonist (IC50 = 7.8 μM).? It displayed robust antitumor activity in B16.F10 melanoma and MC38 colorectal adenocarcinoma mouse models. SR-717 promoted the activation of CD8+ T, natural killer, and dendritic cells as well as promoting antigen cross-priming. It was able to induce PD-L1 expression in THP1 cells and in primary human PBMC’s.
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].
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. |
Chin et al. (2020), Antitumor activity of a systemic STING-activating non-nucleotide cGAMP mimetic; Science 369 993
