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| 5mg |
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| 10mg |
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| 25mg |
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| Targets |
STING (Stimulator of Interferon Genes); STING agonist-12 is a potent activator of the human STING protein. STING is a critical component of the innate immune system that senses cytosolic DNA and triggers the production of type I interferons and other inflammatory cytokines. By activating STING, this compound initiates a strong anti-tumor immune response.
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| ln Vitro |
STING agonist-12 (compound 53) (10 μM) exhibited remarkable pan-polymorphic action against all STING proteins in HEK293T cells, with respective percentages of 92%, 107%, and 92% against R232, H232, and HAQ [1]. When it comes to mouse STING, STING agonist-12 is ineffective [1].
In vitro, STING agonist-12 (10 μM) exhibits remarkable pan-polymorphic action against all STING proteins in HEK293T cells, with respective percentages of 92%, 107%, and 92% against R232, H232, and HAQ variants. It activates the IRF3 reporter with an EC50 of 185.0 nM. It is not active at mouse STING. |
| ln Vivo |
Compound 53, also known as STING agonist-12, has a short terminal half-life and is well absorbed (5 mpk intravenously and 10 mpk orally) [1].
In vivo, STING agonist-12 is well-absorbed with a short terminal half-life. It is administered intravenously at 5 mpk or orally at 10 mpk. As a potent STING activator, it has potential in cancer immunotherapy by stimulating the innate immune system to attack tumors. |
| Enzyme Assay |
In vitro, HEK293T cells are used to assess STING activation. Cells are transfected with various STING constructs and treated with the compound (e.g., 10 μM). Activity is measured using a reporter gene assay for IRF3 activation. The EC50 value of 185 nM is determined from dose-response curves.
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| Cell Assay |
In cell-based assays, HEK293T cells are treated with STING agonist-12. The compound is typically dissolved in DMSO. After incubation, STING pathway activation is measured by assessing the phosphorylation of downstream targets like TBK1 and IRF3, or by using a reporter gene assay.
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| Animal Protocol |
Animal/Disease Models: balb/c (Bagg ALBino) mouse (n=3)[1]
Doses: 5 or 10 mpk Route of Administration: lateral tail vein or po (oral gavage) (pharmacokinetic/PK/PK analysis) Experimental Results: STING agonist-12 (compound 53) pharmacokinetic/PK/PK characteristics in mice [1]. Route dose (mpk) AUC (ng/mL*h) T1/2 (h) Cmax (ng/mL) Vd (mL/kg) F (%) IV 5 1215 1.41 1867 2689 NA PO 10 2090 NA 1723 NA 86 In vivo, STING agonist-12 is administered to animal models via intravenous (5 mpk) or oral (10 mpk) routes. Pharmacokinetic parameters, such as absorption and half-life, are assessed. Efficacy can be evaluated in syngeneic tumor models where STING activation is expected to elicit an anti-tumor immune response. |
| ADME/Pharmacokinetics |
STING agonist-12 has a molecular weight of 490.88 and formula C25H19ClF4N2O2. It is orally active. It should be stored at 4°C, protected from light; in solvent at -80°C for 6 months or -20°C for 1 month.
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| Toxicity/Toxicokinetics |
Specific toxicity data are not extensively documented. As a STING agonist, it may induce inflammatory responses. The compound is for research use only. It should be handled with appropriate safety precautions.
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| References | |
| Additional Infomation |
STING agonist-12 is also known as Compound 53. It is a potent, orally active human STING activator. It is used in cancer immunotherapy research. It is not an FDA-approved drug and is for research use only.
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| Molecular Formula |
C25H19CLF4N2O2
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| Molecular Weight |
490.88
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| Exact Mass |
490.107
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| CAS # |
2259624-71-8
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| PubChem CID |
137367538
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| Appearance |
Light yellow to yellow solid powder
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| LogP |
5.2
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
34
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| Complexity |
759
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| Defined Atom Stereocenter Count |
0
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| SMILES |
N1(CC2=C(F)C=CC=C2Cl)C2=C(C=CC(C(NCC3=C(F)C=C(F)C=C3F)=O)=C2)C(C)(C)C1=O
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| InChi Key |
OEBVYNULNKSONR-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C25H19ClF4N2O2/c1-25(2)17-7-6-13(23(33)31-11-15-20(29)9-14(27)10-21(15)30)8-22(17)32(24(25)34)12-16-18(26)4-3-5-19(16)28/h3-10H,11-12H2,1-2H3,(H,31,33)
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| Chemical Name |
1-(2-chloro-6-fluorobenzyl)-3,3-dimethyl-2-oxo-N-(2,4,6-trifluorobenzyl)indoline-6-carboxamide
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| Synonyms |
C53 C-53 STING Agonist-12
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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 : ~250 mg/mL (~509.29 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 | 2.0372 mL | 10.1858 mL | 20.3716 mL | |
| 5 mM | 0.4074 mL | 2.0372 mL | 4.0743 mL | |
| 10 mM | 0.2037 mL | 1.0186 mL | 2.0372 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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