Size | Price | Stock | Qty |
---|---|---|---|
1mg |
|
||
5mg |
|
||
Other Sizes |
|
Targets |
IC50=0.062 nM
|
---|---|
ln Vitro |
The activity of four major CYP isozymes (CYP1A2, CYP2C9, CYP2C19, and CYP2D6) with IC50 values > 100 μM and CYP3A4 with an IC50 = 4.2 μM is inhibited by STING agonist-17 (compound 4a)[1]. With an EC50 of 2.0 nM, STING agonist-17 (compound 4a) (0-2 μM, 24 hours) stimulates IFN-β secretion[1]. Compound 4a, or STING agonist-17, has the ability to promote the expression of signal transduction factors at 2 nM, 10 nM, and 6 hours [1]. Compound 4a's pharmacokinetic characteristics in vitro[1]. Compound 4a's parameter values are as follows: 1A2 >100.0, 2C9 >100.0, 2C19 >100.0, 2D6 >100.0, and 3A4 4.2 Cardiotoxicity (IC50, μM) hERG patch clamp assay >50.0, Liver microsomal phase I stability mouse (%) 38.7 ± 2.6 human (%) 11.2 ± 2.7 Plasma stability mouse (%) >99 human (%) >99
|
ln Vivo |
In female BALB/c mice with colon cancer originating from CT26 cells, STING agonist-17 (compound 4a) (intravenous injection; 0.015 mg/kg, 1.5 mg/kg; every other day; a week) inhibits the formation of tumors[1]. Compound 4a's pharmacokinetic characteristics in vivo[1]. AUClast (μg •h/mL) 4.20 ± 0.26 AUC∞ (μg·h/mL) >4.78 ± 0.59 Parameter Compound 4a T1/2 (h) 10.54 ± 4.10 Vss (L/kg) >17.74 ± 5.29 CL (L/h/kg) 2.12 ± 0.27
|
Cell Assay |
Western Blot Analysis[1]
Cell Types: THP-1 dual cells Tested Concentrations: 2 nM, 10 nM Incubation Duration: 6 hrs (hours) Experimental Results: Induced phosphorylation of signal transduction factors STING, TBK1, IRF3 and STAT1 at 2 nM. Activated the expression of IFNB gene and IFN stimulated gene (ISG). |
Animal Protocol |
Animal/Disease Models: Female balb/c (Bagg ALBino) mouse aged 6 weeks[1]
Doses: 0.015 mg/kg, 1.5 mg/kg Route of Administration: intravenous (iv) injection ; every other day; a week Experimental Results: Inhibited tumor growth in both doses and caused 57% inhibition at a concentration of 1.5 mg/kg on the 17th day without weight loss. |
References |
[1]. Min Jae Jeon, et al. Development of Potent Immune Modulators Targeting Stimulator of Interferon Genes Receptor. J Med Chem. 2022 Apr 14;65(7):5407-5432.
|
Molecular Formula |
C43H53N13O8
|
---|---|
Molecular Weight |
879.96
|
CAS # |
2816929-47-0
|
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)
|
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 | 1.1364 mL | 5.6821 mL | 11.3642 mL | |
5 mM | 0.2273 mL | 1.1364 mL | 2.2728 mL | |
10 mM | 0.1136 mL | 0.5682 mL | 1.1364 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.