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| Targets |
STING[1]
Stimulator of Interferon Genes (STING). STING agonist-3 trihydrochloride binds directly to the STING protein, forming a dimeric interaction that stabilizes the active conformation. This leads to the recruitment and activation of TBK1 and IRF3, resulting in the transcription of type I interferons and other cytokines. It is more bioavailable than natural CDNs. |
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| ln Vitro |
In human embryonic kidney cells (HEK293T) co-transfected with plasmids expressing STING and the enzyme firefly luciferase driven by the interferon stimulated response element promoter, STING agonist-3 trihydrochloride displays a pEC50 value of 7.5 in activation of STING in cells[1]. In the FRET experiment, STING agonist-3 trihydrochloride shows a pIC50 value of 9.5. The purpose of this competition binding test is to measure a molecule's ability to attach to the human STING C-terminal domain (CTD)[1].
STING agonist-3 (diABZI) is a highly potent STING agonist validated using THP1-Dual cells and other STING reporter systems. It induces the activation of NF-kappaB and IRF-dependent responses, leading to the production of type I interferons. The compound has been shown to inhibit tumor growth in a mouse model of colorectal cancer and to block SARS-CoV-2 infection in primary human airway systems. |
| ln Vivo |
In vivo, treatment with STING agonist-3 significantly inhibits tumor growth in a mouse model of colorectal cancer. It also demonstrates potential in the treatment of SARS-CoV-2 infection through the induction of an effective interferon response. In a mouse model of colorectal cancer, diABZI has been shown to activate STING and produce potent anti-tumor effects.
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| Enzyme Assay |
STING binding assay: Recombinant human STING protein is immobilized on a chip. Increasing concentrations of STING agonist-3 trihydrochloride (0-1000 nM) are injected, and binding is measured by SPR. For functional activation, purified STING and TBK1 are incubated with the agonist (0.01-30 uM) in kinase reaction buffer with ATP. Phosphorylation of STING and TBK1 is detected by Western blotting using phospho-specific antibodies.
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| Cell Assay |
THP1-Dual cell-based assay: THP1-Dual cells (5×10⁵ cells/mL) are seeded in 96-well plates and treated with STING agonist-3 (0.01-30 uM) for 18-24 h at 37degC. Supernatants are collected, and IRF-induced secreted embryonic alkaline phosphatase (SEAP) activity is measured using a colorimetric detection reagent. Alternatively, luciferase activity from an ISG54-Luc reporter is measured. EC50 is calculated by non-linear regression.
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| Animal Protocol |
Colorectal cancer mouse model: C57BL/6 mice are subcutaneously injected with MC38 tumor cells (5×10⁵ cells/mouse). When tumors are established (50-100 mm3), mice receive intratumoral or intraperitoneal injections of STING agonist-3 (10-50 ug/mouse) every 2-3 days. Tumor volume is measured. Tumor-infiltrating lymphocytes are analyzed by flow cytometry, and serum cytokine levels are measured by ELISA.
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| ADME/Pharmacokinetics |
STING agonist-3 (diABZI) has improved pharmacokinetic properties compared to cyclic dinucleotide STING agonists. It is reported to have increased bioavailability and can be administered systemically (intraperitoneally or intravenously). The trihydrochloride salt is water-soluble (2 mg/mL in H2O). The compound has a molecular weight of 959.3 g/mol (trihydrochloride).
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| Toxicity/Toxicokinetics |
Toxicity data for STING agonist-3 are being evaluated. Systemic STING activation can lead to cytokine release syndrome-like effects, including flu-like symptoms, inflammation, and potential tissue damage. Preclinical studies report that diABZI is well-tolerated at effective doses, but safety profiles depend on route of administration and dose frequency. For research use only.
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| References | |
| Additional Infomation |
STING agonist-3 trihydrochloride (diABZI, compound 3) is a research compound that has not yet entered clinical trials. It is a non-nucleotide STING agonist developed to overcome the limitations of cyclic dinucleotides, including poor bioavailability. CAS: 2138299-34-8. For research use only. Store at -20degC, avoid repeated freeze-thaw cycles.
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| Molecular Formula |
C37H45CL3N12O6
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| Molecular Weight |
860.19
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| Related CAS # |
STING agonist-3;2138299-29-1
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| Appearance |
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: (1). This product requires protection from light (avoid light exposure) during transportation and storage. (2). Please store this product in a sealed and protected environment (e.g. under nitrogen), 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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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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 | 1.1625 mL | 5.8127 mL | 11.6253 mL | |
| 5 mM | 0.2325 mL | 1.1625 mL | 2.3251 mL | |
| 10 mM | 0.1163 mL | 0.5813 mL | 1.1625 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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