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SR-717

  Cat. No.:  DC39030   Featured
Chemical Structure
2375421-09-1
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Field of application
SR-717 is a non-nucleotide, small-molecule STING agonist and functions as a direct cyclic guanosine monophosphate-adenosine monophosphate (cGAMP) mimetic that induces the same "closed" conformation of STING.SR-717 functions as a direct cyclic guanosine mo
Chemicals PropertiesBiological activity COA & MSDSRelated productsDatasheet
Cas No.: 2375421-09-1
Chemical Name: SR-717
Synonyms: Lithium 4,5-difluoro-2-({[6-(1H-imidazol-1-yl)-3-pyridazinyl]carbonyl}amino)benzoate;SR-717;Benzoic acid, 4,5-difluoro-2-[[[6-(1H-imidazol-1-yl)-3-pyridazinyl]carbonyl]amino]-, lithium salt (1:1);Lithium;4,5-difluoro-2-[(6-imidazol-1-ylpyridazine-3-carbonyl)amino]benzoate;Lithium 2-(6-(1H-imidazol-1-yl)pyridazine-3-carboxamido)-4,5-difluorobenzoate;AVD42109;E73475;SR-717 lithium
SMILES: FC1=C(C([H])=C(C(=O)[O-])C(=C1[H])N([H])C(C1C([H])=C([H])C(=NN=1)N1C([H])=NC([H])=C1[H])=O)F.[Li+]
Formula: C15H8F2LiN5O3
M.Wt: 351.1935
Purity: >98%
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Publication: [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
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].
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.
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].
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MSDS_20444_DC39030_2375420-34-9
COA
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Cat. No. Product name Field of application
DC60500 NVS-STG2 NVS-STG2 is a small molecule STING agonist with AC50 of 5.2 μM. NVS-STG2 induces the high-order oligomerization of human STING by binding to a pocket between the transmembrane domains of the neighboring STING dimers and elicit potent STING-mediated immune responses in cells and antitumor activities in animal models.
DC60034 STING inhibitor-1 STING inhbiitor, which inhibited the activation of the STING signal pathway and to prevent or treat a STING-​mediated disease.
DC60033 STING INHIBITOR-2 STING inhbiitor, which inhibited the activation of the STING signal pathway and to prevent or treat a STING-​mediated disease.
DC39220 STING agonist compound 17 STING agonist compound 17 is a selective stimulator of interferon genes (STING) receptor agonist.
DC39210 MSA-2 analogue MSA-2 analogue is an orally available human STING agonist.
DC39031 MSA-2 MSA-2 is an orally available human STING agonist.MSA-2 is bound to STING as a noncovalent dimer. Extensive experimental analysis indicates that MSA-2 predimerization is required for binding. Acidic tumor microenvironments favor permeable, uncharged MSA-2.
DC39030 SR-717 SR-717 is a non-nucleotide, small-molecule STING agonist and functions as a direct cyclic guanosine monophosphate-adenosine monophosphate (cGAMP) mimetic that induces the same "closed" conformation of STING.SR-717 functions as a direct cyclic guanosine mo
DC72041 BSP16 BSP16 is a potent, orally active stimulator of interferon genes (STING) agonist. BSP16 can selectively stimulate the STING pathway. BSP16 can be used for the research of cancer.
DC50039 3'3'-cGAMP (sodium salt) 3’3’-cGAMP Fluorinated (c-[2'FdGMP]-[2'FdAMP]) is a synthetic analog of cyclic guanosine monophosphate- adenosine monophosphate (cyclic GMP-AMP, cGAMP) with a fluorine atom at 2’ position of the nucleosides. 3’3’-cGAMP is a cyclic di-nucleotide produced by bacteria. It is also referred to as "canonical" cGAMP due the presence of the classical 3’-5’ phosphodiester linkages between the guanosine and the adenosine. It has been reported that cGAMP binds STING (stimulator of IFN genes) and subsequently induces TBK1-IRF3-dependent production of IFN-β [1]. The incorporation of fluorine into biologically active molecules is commonly used in medicinal chemistry to improve their metabolic stability or to modulate physicochemical properties such as lipophilicity [2, 3]. Moreover, the introduction of a fluorine atom can change the biological activities of a molecule. Interestingly, when used at low concentrations in various cellular assays, 3’3’-cGAMP Fluorinated induces higher levels of type I IFNs than does cGAMP. STING ligands such as cGAMP induce type I IFNs and activate interferon stimulated genes (ISG) through IRFs. To facilitate their study, InvivoGen has developed stable reporter cells in two well established immune cell models: THP-1 human monocytes and RAW 264.7 murine macrophages. These cells express a reporter gene (SEAP or Lucia luciferase), under control of an IRF-inducible promoter.
DC48024 cGAMP diammonium cGAMP (Cyclic GMP-AMPP) diammonium functions as an endogenous second messenger in metazoans and triggers interferon production in response to cytosolic DNA. cGAMP diammonium activates stimulator of interferon genes (STING), which activates a signaling cascade leading to the production of type I interferons and other immune mediators.
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