| Size | Price | Stock | Qty |
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| 1mg |
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| Other Sizes |
| Targets |
Stimulator of Interferon Genes (STING). STING agonist-8 dihydrochloride binds to and activates the STING protein, a key adaptor in the cytosolic DNA sensing pathway. Activation triggers the phosphorylation of TBK1 and IRF3, leading to the production of type I interferons (IFN-alpha/beta) and pro-inflammatory cytokines, which promote anti-tumor immunity.
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| ln Vitro |
STING agonist-8 dihydrochloride is a potent activator of the STING pathway with an EC50 of 27 nM in THP1-Dual KI-hSTING-R232 reporter cells. Activation of STING leads to the induction of type I interferons and pro-inflammatory cytokines in a concentration-dependent manner. The compound is more potent than the natural STING ligand 2'3'-cGAMP.
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| ln Vivo |
In vivo, STING agonists such as agonist-8 dihydrochloride have been shown to inhibit tumor growth in syngeneic mouse models. Intratumoral injection leads to activation of the STING pathway within the tumor microenvironment, promoting infiltration and activation of CD8+ T cells and natural killer cells, resulting in tumor regression and abscopal effects.
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| Enzyme Assay |
STING binding and activation assay (non-cell-based): Purified STING protein is incubated with increasing concentrations of STING agonist-8 dihydrochloride (0-1000 nM) in binding buffer. Compound binding is measured by surface plasmon resonance (SPR) or thermal shift assay. For activation, recombinant STING protein is incubated with the compound in the presence of TBK1 and ATP, and phosphorylation of STING and TBK1 is detected by Western blotting.
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| Cell Assay |
THP1-Dual cell-based reporter assay: THP1-Dual cells expressing a STING-inducible reporter gene (IRF-inducible SEAP or ISG54-Luc) are seeded in 96-well plates (2×10⁵ cells/well). STING agonist-8 dihydrochloride (0-1000 nM) is added to the cells and incubated for 18-24 h at 37degC. Reporter activity (SEAP or luciferase) is measured by adding a detection reagent and reading absorbance or luminescence. EC50 (27 nM) is calculated by non-linear regression.
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| Animal Protocol |
Syngeneic tumor model: C57BL/6 mice are inoculated subcutaneously with STING-sensitive tumor cells (e.g., B16-F10 melanoma or CT26 colon carcinoma). When tumors reach 50-100 mm3, STING agonist-8 dihydrochloride is administered intratumorally at doses of 10-100 ug per mouse, every 2-3 days for a total of 3-5 doses. Tumor volume is measured every 2-3 days. Tumor-infiltrating lymphocytes are analyzed by flow cytometry.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for STING agonist-8 dihydrochloride are limited. As a small molecule (MW 871.82), it is typically administered intratumorally to achieve high local concentrations. Systemic exposure following intratumoral injection is minimal, reducing the risk of systemic cytokine-related toxicities. The compound is soluble in DMSO and can be formulated in appropriate vehicles for injection.
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| Toxicity/Toxicokinetics |
Toxicity data for STING agonist-8 dihydrochloride are being evaluated in preclinical studies. Systemic administration of STING agonists can lead to cytokine release syndrome (CRS)-like toxicities, including fever, hypotension, and systemic inflammation. At high doses, organ toxicity may occur. The compound is intended for research use only and not for human therapeutic applications.
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| References | |
| Additional Infomation |
STING agonist-8 dihydrochloride (5-AB) is a research compound that has not entered clinical trials or received regulatory approval for human use. It is a member of the amidobenzimidazole (ABZI) family of STING agonists. The compound is for research purposes only and should be stored at -20degC, protected from light and moisture.
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| Molecular Formula |
C41H48CL2N14O4
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|---|---|
| Molecular Weight |
871.82
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| Related CAS # |
STING agonist-8;2745723-90-2
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| Appearance |
White to off-white solid powder
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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: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| 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 (~5.74 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1 mg/mL (1.15 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 10.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.1470 mL | 5.7351 mL | 11.4703 mL | |
| 5 mM | 0.2294 mL | 1.1470 mL | 2.2941 mL | |
| 10 mM | 0.1147 mL | 0.5735 mL | 1.1470 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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