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SR-717

Names

[ CAS No. ]:
2375421-09-1

[ Name ]:
SR-717

Biological Activity

[Description]:

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].

[Related Catalog]:

Research Areas >> Cancer
Research Areas >> Inflammation/Immunology
Signaling Pathways >> Immunology/Inflammation >> STING

[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]

[1]. Emily N Chin, et al. Antitumor activity of a systemic STING-activating non-nucleotide cGAMP mimetic. Science. 2020 Aug 21;369(6506):993-999.

Chemical & Physical Properties

[ Molecular Formula ]:
C15H8F2LiN5O3

[ Molecular Weight ]:
351.19

[ Storage condition ]:
-20°C


Related Compounds