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| Targets |
STING agonist-16 specifically targets the stimulator of interferon genes (STING), a transmembrane adaptor protein located on the endoplasmic reticulum that plays a central role in the innate immune response to cytosolic DNA. Upon binding to STING, STING agonist-16 triggers the activation of the TBK1/IRF3 signaling axis, leading to the phosphorylation and nuclear translocation of IRF3, which drives the expression of type I interferons (IFN-alpha, IFN-beta) and other pro-inflammatory cytokines. It acts as a specific stimulator of interferon genes.
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| ln Vitro |
No evident cytotoxic effect on cells (THP1) STING agonist-16 (1a) (0-100 μM, 6 hours) increases IFNβ, CXCL-10, and IL-6 mRNA expression in human myeloid leukemia monocytes in a dose-dependent manner up to 100 μM [1]. The phosphorylation of STING, TANK-binding kinase 1 (TBK1), and interferon regulatory factor 3 (IRF3) is considerably induced in THP1 cells by STING agonist-16 (1a) (50 μM, 2 h) [1]. The EC50 value of 2'3'-cGAMP is 9.212 μM, whereas STING agonist-16 (1a) activates secreted alkaline phosphatase (SEAP) in a dose-dependent manner at 16.77 μM [1].
In vitro, STING agonist-16 activates the STING pathway in a dose-dependent manner. In THP1 human monocytic cells, treatment with STING agonist-16 (0-100 uM) results in the activation of secreted alkaline phosphatase (SEAP) under the control of an IRF-inducible promoter, with a half-maximal effective concentration (EC50) of 16.77 uM in reporter cell assays. Importantly, the compound exhibits no evident cytotoxic effect on cells (THP1) at concentrations up to 100 uM. It promotes type I interferon production and enhances immune cell activation, confirming its role as a potent STING agonist for studying innate immunity. |
| ln Vivo |
In vivo, STING agonist-16 is a potential tool for antiviral and antitumor applications. As a STING agonist, it activates the intrinsic immune response and promotes the production of type I interferons, which are critical for combating viral infections and enhancing anti-tumor immunity. By activating the STING pathway, the compound induces a robust type I interferon response that can inhibit viral replication and promote the activation of cytotoxic T lymphocytes (CTLs) against tumor cells. This makes it a potential candidate for cancer immunotherapy and antiviral therapy. Detailed in vivo efficacy data is available in the primary literature.
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| Enzyme Assay |
For non-cell-based binding assays, a standard protocol for assessing STING activation uses a competitive binding assay with the natural STING ligand, cyclic di-GMP (c-di-GMP). Recombinant human STING protein is immobilized on a 96-well plate. Varying concentrations of STING agonist-16 (0.1-1000 uM) are added in the presence of a fixed concentration of a biotinylated STING ligand (e.g., 2',3'-cGAMP). After incubation and washing, bound biotinylated ligand is detected using streptavidin-HRP and a chemiluminescent substrate. The IC50 for competition is calculated from the dose-response curve. Alternatively, a differential scanning fluorimetry (DSF) assay measures the thermal stabilization of STING protein upon ligand binding.
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| Cell Assay |
For in vitro cell-based assays, THP1-Dual cells (THP1 monocytes stably transfected with an IRF-inducible SEAP reporter) are seeded in 96-well plates at 5 × 10^4 cells/well. Cells are treated with varying concentrations of STING agonist-16 (0-100 uM) for 18-24 hours at 37degC in 5% CO2. After incubation, 20 uL of cell supernatant is transferred to a new 96-well plate containing 180 uL of QUANTI-Blue reagent (a SEAP detection substrate). The plate is incubated at 37degC for 2-3 hours, and absorbance is measured at 620-655 nm. The EC50 for STING activation is calculated. For analysis of cytokine production, supernatants are collected after 24 hours and analyzed for IFN-beta, IL-6, and TNF-alpha by ELISA.
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| Animal Protocol |
For in vivo animal studies, a syngeneic mouse tumor model (e.g., CT26 colon carcinoma or B16-F10 melanoma) can be used. Female BALB/c mice are subcutaneously injected with 5 × 10^5 CT26 tumor cells. When tumors reach 50-100 mm3 (day 7-10), mice are treated with STING agonist-16 via intratumoral injection at doses of 10-100 ug per tumor, administered every 3 days for a total of 3-4 doses. Control animals receive vehicle (e.g., 5% DMSO in PBS). Tumor volume is measured every 2-3 days by calipers. For assessment of immune responses, tumors and draining lymph nodes are harvested at day 14 for flow cytometry analysis of CD8+ T cell infiltration and activation (CD69, Granzyme B). Serum is collected for cytokine analysis (IFN-beta, IFN-gamma, IL-6, TNF-alpha) by ELISA.
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| ADME/Pharmacokinetics |
STING agonist-16 is a small molecule with a molecular weight of 396.23 g/mol and good cell membrane permeability (cLogP ~3.5-4.5). The compound is soluble in DMSO (5 mg/mL, 12.62 mM) but has poor aqueous solubility, requiring the use of co-solvents (e.g., DMSO/PEG400/saline) for in vivo administration. The pharmacokinetic profile in mice is not publicly available, but as a small molecule, it is expected to be rapidly absorbed and distributed following intratumoral or intraperitoneal administration. The elimination half-life is likely short (1-2 hours), requiring frequent dosing for sustained pathway activation.
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| Toxicity/Toxicokinetics |
Specific toxicology data for STING agonist-16 is not publicly available, as it is a preclinical research compound. In cell viability assays using THP1 cells, the compound exhibits no evident cytotoxic effect at concentrations up to 100 uM, indicating a favorable safety window. However, STING activation is a potent driver of inflammation, and systemic administration of STING agonists can cause cytokine release syndrome (CRS), characterized by fever, hypotension, and tissue damage due to excessive production of type I interferons and pro-inflammatory cytokines. Therefore, careful dose optimization is required for in vivo applications. The compound is not approved for human use.
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| References | |
| Additional Infomation |
STING agonist-16 is a research compound and is not approved for clinical use. It is a valuable chemical tool for studying the role of the cGAS-STING pathway in innate immunity, antiviral defense, and cancer immunotherapy. STING is a key mediator of the immune response to cytosolic DNA, and its activation by STING agonist-16 leads to the production of type I interferons, which are essential for host defense against viruses and for priming anti-tumor CD8+ T cell responses. This compound is for research use only and is not intended for human or veterinary applications. The compound is also known as STING Agonist 1a.
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| Molecular Formula |
C19H11CL2N5O
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|---|---|
| Molecular Weight |
396.229541063309
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| Exact Mass |
395.034
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| CAS # |
652142-94-4
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| PubChem CID |
1002560
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| Appearance |
Off-white to light brown solid powder
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| Density |
1.6±0.1 g/cm3
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| Index of Refraction |
1.772
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| LogP |
4.4
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
27
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| Complexity |
542
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| Defined Atom Stereocenter Count |
0
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| SMILES |
COC1=CC2=CC(=C(N=C2C=C1)Cl)C3=NN=C4N3C5=CC=CC=C5N=C4Cl
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| InChi Key |
ABGPUQXRCXUIFE-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C19H11Cl2N5O/c1-27-11-6-7-13-10(8-11)9-12(16(20)22-13)18-24-25-19-17(21)23-14-4-2-3-5-15(14)26(18)19/h2-9H,1H3
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| Chemical Name |
4-chloro-1-(2-chloro-6-methoxyquinolin-3-yl)-[1,2,4]triazolo[4,3-a]quinoxaline
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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 |
| 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 : ~5 mg/mL (~12.62 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 | 2.5238 mL | 12.6189 mL | 25.2379 mL | |
| 5 mM | 0.5048 mL | 2.5238 mL | 5.0476 mL | |
| 10 mM | 0.2524 mL | 1.2619 mL | 2.5238 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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