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| 1mg |
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| 5mg |
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| Other Sizes |
| Targets |
STING agonist-22 specifically targets the STING protein, activating the STING signaling pathway. Upon binding, STING dimerizes and translocates to the Golgi, where it phosphorylates TBK1. TBK1 then phosphorylates IRF3, which translocates to the nucleus to induce expression of type I interferons (IFN-alpha/beta) and other pro-inflammatory cytokines. This activation enhances both innate and adaptive immune responses.
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| ln Vitro |
THP-1 cells' innate immunological responses are quickly and strongly activated by STING agonist-22 (CF501) [1].
In vitro, STING agonist-22 acts as an effective non-nucleotide STING agonist. It induces the production of type I interferon (IFN-I) response and proinflammatory cytokines in STING-expressing cells. The compound triggers downstream signaling including IRF3 phosphorylation and nuclear translocation, leading to increased expression of ISGs. It has been shown to be a potent activator in primary immune cells. |
| ln Vivo |
In mice with an appropriate safety profile, STING agonist-22 (CF501) stimulates innate immunity robustly but momentarily[1].
In vivo, STING agonist-22 can be utilized as an adjuvant to enhance the original protein vaccine, resulting in effective, broad, and long-term immune protection. It is used for SARS-CoV-2 variants and sarbecovirus diseases research. STING agonist-22 (CF501) is an adjuvant that induces type I interferon (IFN-I) responses and proinflammatory cytokine production through activation of STING. |
| Enzyme Assay |
The specific protocol for STING binding uses a homogeneous time-resolved fluorescence (HTRF) competition binding assay. Recombinant human STING protein (His-tagged) is incubated with a Europium-labeled anti-His antibody (donor) and a fluorescent-labeled small molecule STING agonist (acceptor). STING agonist-22 is serially diluted (0.1 nM to 100 uM) and added to the mixture. After 60 minutes, HTRF signal (665/620 nm ratio) is measured. The IC50 is calculated from the competition curve.
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| Cell Assay |
For in vitro cellular assays, THP-1 cells (human monocytic cell line) are seeded in 96-well plates. Cells are treated with STING agonist-22 (CF501) at concentrations ranging from 0.1-100 uM for 6-24 hours. Cell culture supernatants are harvested, and the levels of IFN-beta, TNF-alpha, and IL-6 are quantified using a multiplex ELISA kit. To assess STING pathway activation, cells are lysed and analyzed by Western blotting using antibodies against p-TBK1 (Ser172) and p-IRF3 (Ser396).
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| Animal Protocol |
Animal/Disease Models: balb/c (Bagg ALBino) mouse (female, six weeks old)[1]
Doses: 20, 75 μg Route of Administration: intramuscular (im) injection Experimental Results: Although innate immunity was activated only transiently by CF501, it should be sufficient to stimulate the required humoral and cellular immune responses. The half-life of CF501 was 0.5 h and there was no detectable CF501 in the plasma after 2 h of the injection. In an in vivo vaccine adjuvant protocol, female BALB/c mice (6-8 weeks old) are immunized intramuscularly (IM) with a protein antigen (e.g., SARS-CoV-2 spike protein RBD, 10 ug) mixed with STING agonist-22 (CF501, 10-50 ug) in a total volume of 50 uL PBS. A booster immunization is administered on day 14 or day 21. Blood samples are collected on days 0, 14, 21, and 28. Serum antibody titers (IgG, IgG1, IgG2a) are measured by ELISA. Splenocytes are collected at study termination for ELISpot assays to measure IFN-gamma-secreting T cells. |
| ADME/Pharmacokinetics |
Specific pharmacokinetic data for STING agonist-22 is not widely published. As a non-nucleotide small molecule STING agonist, it is expected to have moderate metabolic stability and suitable properties for intramuscular administration as a vaccine adjuvant. The compound is likely to have a relatively short residence time at the injection site, with rapid clearance from the systemic circulation to avoid systemic toxicity.
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| Toxicity/Toxicokinetics |
Toxicology data for STING agonist-22 is not extensively documented. As a vaccine adjuvant, the compound is intended for limited, localized administration (intramuscular injection) rather than chronic systemic exposure. Preclinical safety assessment would include local tolerance studies at the injection site (histopathological examination) and systemic toxicology studies in rodents, including evaluation of cytokine levels (to monitor for cytokine release syndrome).
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| References | |
| Additional Infomation |
STING agonist-22 (CF501) is a research-grade compound and is not approved for human use. Its molecular formula is C40H48N14O6 with a molecular weight of 820.90. It is a potent non-nucleotide STING agonist. STING agonist-22 is an adjuvant that induces type I interferon (IFN-I) responses and proinflammatory cytokine production through activation of STING. It could be utilized as an adjuvant to enhance the original protein vaccine, resulting in effective, broad, and long-term immune protection for SARS-CoV-2 variants and sarbecovirus diseases research.
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| Molecular Formula |
C40H48N14O6
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| Molecular Weight |
820.899326324463
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| Exact Mass |
820.388
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| CAS # |
2408723-12-4
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| PubChem CID |
146295210
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| Appearance |
White to off-white solid powder
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| LogP |
1.2
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
12
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| Rotatable Bond Count |
17
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| Heavy Atom Count |
60
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| Complexity |
1520
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C12N(C/C=C/CN3C(NC(C4N(CC)N=C(C)C=4)=O)=NC4=CC(C(N)=O)=CC(OCCCN5CCOCC5)=C43)C(NC(C3N(CC)N=C(C)C=3)=O)=NC1=CC(C(N)=O)=CN=2
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| InChi Key |
HYWPJLWOHDVWMY-BQYQJAHWSA-N
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| InChi Code |
InChI=1S/C40H48N14O6/c1-5-53-30(18-24(3)48-53)37(57)46-39-44-28-20-26(34(41)55)22-32(60-15-9-10-50-13-16-59-17-14-50)33(28)51(39)11-7-8-12-52-36-29(21-27(23-43-36)35(42)56)45-40(52)47-38(58)31-19-25(4)49-54(31)6-2/h7-8,18-23H,5-6,9-17H2,1-4H3,(H2,41,55)(H2,42,56)(H,44,46,57)(H,45,47,58)/b8-7+
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| Chemical Name |
3-[(E)-4-[5-carbamoyl-2-[(2-ethyl-5-methylpyrazole-3-carbonyl)amino]-7-(3-morpholin-4-ylpropoxy)benzimidazol-1-yl]but-2-enyl]-2-[(2-ethyl-5-methylpyrazole-3-carbonyl)amino]imidazo[4,5-b]pyridine-6-carboxamide
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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: 100 mg/mL (121.82 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 | 1.2182 mL | 6.0909 mL | 12.1818 mL | |
| 5 mM | 0.2436 mL | 1.2182 mL | 2.4364 mL | |
| 10 mM | 0.1218 mL | 0.6091 mL | 1.2182 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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