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| Targets |
STING agonist-7 selectively targets mouse STING, with minimal binding affinity for human STING. The compound binds to STING, leading to activation of the downstream TBK1/IRF3 signaling cascade and subsequent induction of type I interferons. The molecular basis for species selectivity is due to differences in the amino acid residues within the STING ligand-binding pocket between mouse and human.
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| ln Vitro |
Compound 11, also known as STING agonist-7, exhibits activity in biochemical tests but inactivity in cellular reporter experiments [1].
In vitro, STING agonist-7 is a non-nucleotide STING agonist that selectively binds mouse STING but not human STING. This has been confirmed in cell-based assays using mouse and human cell lines. The compound penetrates cell membranes poorly, which may limit its activity in certain in vitro settings but can be an advantage for localized in vivo applications. It induces IFN-beta production in mouse cells with an EC50 value not specifically detailed, but its activity is selective for mouse STING. |
| ln Vivo |
In vivo, STING agonist-7 has shown activity in mouse tumor models. It is widely used in cancer immunotherapy research for enhancing T cell infiltration and overcoming immune evasion in solid tumors. It also holds promise in vaccine adjuvant development and in studying autoimmune or inflammatory responses driven by cyclic dinucleotide signaling. The compound's selectivity for mouse STING allows for the investigation of STING-specific effects without confounding activity on human STING.
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| Enzyme Assay |
The specific in vitro binding protocol for STING agonist-7 uses a thermal shift assay (differential scanning fluorimetry) to measure binding and stabilization of STING protein. Recombinant mouse STING protein (1-340) is incubated with a serial dilution of STING agonist-7 (1-100 uM) in PBS containing SYPRO Orange dye. The temperature is increased from 25degC to 95degC at a rate of 1degC per minute. Fluorescence changes are monitored, and the melting temperature (Tm) is calculated. A positive Tm shift indicates binding and stabilization of mouse STING. No shift is observed with human STING protein.
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| Cell Assay |
For in vitro cellular assays, mouse RAW264.7 macrophages (or primary mouse peritoneal macrophages) are seeded in 96-well plates. The cells are treated with STING agonist-7 at concentrations ranging from 1-100 uM for 6-24 hours. Cell supernatants are collected and mouse IFN-beta is quantified by ELISA. As a negative control, human THP-1 cells are treated in parallel and show no significant IFN-beta induction. To assess cell membrane permeability, intracellular levels of the compound can be measured by LC-MS/MS.
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| Animal Protocol |
An in vivo protocol for STING agonist-7 uses a B16-F10 melanoma model in C57BL/6 mice. Mice are inoculated subcutaneously with 1×10⁶ B16-F10 cells. When tumors reach 50-100 mm3 (day 7-10), mice receive intratumoral injections of STING agonist-7 (50-200 ug in 30 uL 10% DMSO in PBS) on days 7, 9, 11, and 13. Tumor volumes are measured with calipers every 2 days. At the end of the study, tumors are harvested and digested for flow cytometry analysis of CD8+ T-cell infiltration. The species selectivity ensures that observed effects are mediated through mouse STING.
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| ADME/Pharmacokinetics |
Specific pharmacokinetic data for STING agonist-7 is not available. The compound is noted to penetrate cell membranes poorly, which may impact its absorption and distribution properties. For in vivo studies, it is typically administered intratumorally to ensure adequate local concentrations at the target site. Formulations may include DMSO or co-solvents to enhance solubility and delivery. The poor membrane permeability may be an advantage for localized rather than systemic applications.
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| Toxicity/Toxicokinetics |
Toxicology data for STING agonist-7 is not well-documented. As a STING agonist that does not activate human STING, its toxicity profile in animal models is relevant primarily for understanding species-specific effects. Standard safety assessment in mice would include monitoring for signs of systemic inflammation (elevated cytokines, weight loss, fever) following intratumoral administration. No significant toxicity at efficacious doses has been reported in the literature.
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| References | |
| Additional Infomation |
STING agonist-7 is a research-grade chemical and is not approved for clinical use. Its molecular formula is C17H12N4O4 with a molecular weight of 336.30. It is a non-nucleotide STING agonist that binds selectively to mouse STING but not human STING. STING agonist-7 penetrates cell membranes poorly. It is widely used in cancer immunotherapy research, particularly for enhancing T cell infiltration and overcoming immune evasion in solid tumors. It also holds promise in vaccine adjuvant development and in studying autoimmune or inflammatory responses driven by cyclic dinucleotide signaling.
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| Molecular Formula |
C17H12N4O4
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| Molecular Weight |
336.3015832901
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| Exact Mass |
336.085
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| CAS # |
2767442-46-4
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| PubChem CID |
162540443
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| Appearance |
Light brown to brown solid powder
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| LogP |
1.1
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
25
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| Complexity |
531
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1=CC2=C(C(=C1)C(=O)O)OC(=C2)CNC(=O)C3=C4N=CC=CN4N=C3
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| InChi Key |
BICDHWPHEXMVAT-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C17H12N4O4/c22-16(13-9-20-21-6-2-5-18-15(13)21)19-8-11-7-10-3-1-4-12(17(23)24)14(10)25-11/h1-7,9H,8H2,(H,19,22)(H,23,24)
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| Chemical Name |
2-[(pyrazolo[1,5-a]pyrimidine-3-carbonylamino)methyl]-1-benzofuran-7-carboxylic acid
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: 62.5 mg/mL (185.85 mM)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.9735 mL | 14.8677 mL | 29.7354 mL | |
| 5 mM | 0.5947 mL | 2.9735 mL | 5.9471 mL | |
| 10 mM | 0.2974 mL | 1.4868 mL | 2.9735 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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