STING agonist-17
Based on 1 Customer Validation
STING agonist-17 (compound 4a) is a potent STING agonist with an IC50 value of 0.062 nM. STING agonist-17 has anti-cancer activity for tumor immunization.
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- Pureté: 96.15%
- CAS No.: 2816929-47-0
- Formule: C43H53N13O8
- Masse moléculaire:879.96
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
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Immunology/Inflammation Compound Library
HY-L007
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Anti-Cancer Compound Library
HY-L025
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Small Molecule Immuno-Oncology Compound Library
HY-L031
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Heterocyclic Compound Library
HY-L138
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Immunopotentiator Compound Library
HY-L172
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Bioactive Compound Library Max
HY-L181
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MCE Bioactive Compound Library
HY-L001V
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Bioactive Compound Library
HY-L001
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High-Throughput Bioactive Compound Library
HY-L205
Activité biologique
IC50=0.062 nM
STING agonist-17 (compound 4a) inhibits the activity of four major CYP isozymes (CYP1A2, CYP2C9, CYP2C19 and CYP2D6) with IC50 values > 100 μM and for CYP3A4 with an IC50 = 4.2 μM[1]. STING agonist-17 (compound 4a) (0-2 μM, 24 hours) induces IFN-β secretion with the EC50 of 2.0 nM[1]. STING agonist-17 (compound 4a) (2 nM, 10 nM, 6 hours) can induce the expression of signal transduction factors[1]. The pharmacokinetic parameters of Compound 4a in vitro[1].
| Parameter | Compound 4a |
| CYP inhibition (IC50, μM) | |
| 1A2 | >100.0 |
| 2C9 | >100.0 |
| 2C19 | >100.0 |
| 2D6 | >100.0 |
| 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 |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:THP-1 dual cells
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Concentration:2 nM, 10 nM
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Incubation Time:6 hours
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Result: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).
| 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 |
| AUClast (μg h/mL) | 4.20 ± 0.26 |
| AUC∞ (μg h/mL) | >4.78 ± 0.59 |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female BALB/c mice aged 6 weeks[1]
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Dosage:0.015 mg/kg, 1.5 mg/kg
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Administration:Intravenous injection; every other day; a week
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Result: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.
Chemical Information
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CAS No. 2816929-47-0
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Appearance Solid
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Masse moléculaire 879.96
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Formule C43H53N13O8
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Color Off-white to light yellow
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SMILES
CCN1N=C(C=C1C(NC2=NC3=C(N2C/C=C/CN4C(NC(C5=CC(C)=NN5CC)=O)=NC6=CC(C(N)=O)=CC(OCCCNC(OC(C)(C)C)=O)=C64)C(OC)=CC(C(N)=O)=C3)=O)C
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvant et solubilité
DMSO : 100 mg/mL (113.64 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: 2.5 mg/mL (2.84 mM); Clear solution; Need ultrasonic
This protocol yields a clear solution of 2.5 mg/mL.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureté et documentation
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Fiche technique (283 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Instruction de manipulation (2659 KB)
Références
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.1364 mL | 5.6821 mL | 11.3642 mL | 28.4104 mL |
| 5 mM | 0.2273 mL | 1.1364 mL | 2.2728 mL | 5.6821 mL | |
| 10 mM | 0.1136 mL | 0.5682 mL | 1.1364 mL | 2.8410 mL | |
| 15 mM | 0.0758 mL | 0.3788 mL | 0.7576 mL | 1.8940 mL | |
| 20 mM | 0.0568 mL | 0.2841 mL | 0.5682 mL | 1.4205 mL | |
| 25 mM | 0.0455 mL | 0.2273 mL | 0.4546 mL | 1.1364 mL | |
| 30 mM | 0.0379 mL | 0.1894 mL | 0.3788 mL | 0.9470 mL | |
| 40 mM | 0.0284 mL | 0.1421 mL | 0.2841 mL | 0.7103 mL | |
| 50 mM | 0.0227 mL | 0.1136 mL | 0.2273 mL | 0.5682 mL | |
| 60 mM | 0.0189 mL | 0.0947 mL | 0.1894 mL | 0.4735 mL | |
| 80 mM | 0.0142 mL | 0.0710 mL | 0.1421 mL | 0.3551 mL | |
| 100 mM | 0.0114 mL | 0.0568 mL | 0.1136 mL | 0.2841 mL |
STING agonist-17 Related Classifications
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