STING agonist-45
Based on 1 Customer Validation
STING agonist-45 is a selective STING agonist (EC50 = 0.28 μM). STING agonist-45 activates the innate immune response through the cGAS-STING pathway, upregulating key markers such as p-TBK1 and IRF3. STING agonist-45 exhibits robust STING activation in human peripheral blood mononuclear cells (PBMCs), inducing the production of type I interferons (such as IFN-β) and downstream cytokines (such as TNF-α and IL-6). STING agonist-45 enhances anti-tumor immunity, inhibits tumor growth, and increases CD8+ T cell infiltration in mouse models. STING agonist-45 is promising for the study of STING-related diseases.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza : 99.10%
- No. CAS: 2361424-97-5
- Fòrmula: C21H26N6O4
- Peso molecular:426.47
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
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Actividad biológica
Descripciòn
In Vitro
STING agonist-45 (Compound 12L) (24 h) induces reporter signal in RAW 264.7 cells with an EC50 value of 5.22 µM [1].
STING agonist-45 (24 h) shows obvious cytotoxicity against THP1 cells[1].
STING agonist-45 (24 h) bind to carboxy terminal domain (CTD) of various hSTING alleles (IC50 = 8.97 µM) and mSTING (IC50 = 4.35 µM)[1].
STING agonist-45 (Example 1) (24 h) stimulates the production of CXCL10 (IP10) cytokines in THP1 cells, with an EC50 value of 1.6 µM[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Parmacokinetics
| Species | Dose | Route | T1/2 | AUC0-t | AUC0-∞ | CL | MRT0-∞ | Vss |
|---|---|---|---|---|---|---|---|---|
| Mice[1] | 10 mg/kg | i.v. | 1.13 h | 3820 ng·h/mL | 3833 ng·h/mL | 43.8 mL/min/kg | 0.894 h | 2377 mL/kg |
In Vivo
STING agonist-45 (10 mg/kg, i.v., once a day, 7 days) reduces tumor volume, prolongs the survival time in B16.F10 tumor-bearing C57BL/6 mice model[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6 mice (6-8 weeks old) model[1]
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Dosage:3, 10, 30 mg/kg
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Administration:i.v., once a day, 4 days
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Result:Dose-dependent induced IFN-β protein.
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Animal Model:B16.F10 tumor-bearing (105) C57BL/6 mice (6-8 weeks old) model[1]
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Dosage:10 mg/kg
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Administration:i.v., once a day, 7 days
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Result:Reduced tumor volume, prolonged the survival time.
Ensayo clínico
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 2361424-97-5
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Appearance Solid
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Peso molecular 426.47
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Fòrmula C21H26N6O4
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Color White to light yellow
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SMILES
O=C(C1=CC2=C(C(OC3COC3)=C1)N(CCC)C(NC(C4=CC(C)=NN4CC)=O)=N2)N
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvente y solubilidad
In Vitro:
DMSO : 100 mg/mL (234.48 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)
In Vivo:
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.
In Vivo Dissolution Calculator
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.
Pureza y Documentación
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Ficha de datos (276 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instrucciones de manejo (2659 KB)
Referencias
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 | 2.3448 mL | 11.7242 mL | 23.4483 mL | 58.6208 mL |
| 5 mM | 0.4690 mL | 2.3448 mL | 4.6897 mL | 11.7242 mL | |
| 10 mM | 0.2345 mL | 1.1724 mL | 2.3448 mL | 5.8621 mL | |
| 15 mM | 0.1563 mL | 0.7816 mL | 1.5632 mL | 3.9081 mL | |
| 20 mM | 0.1172 mL | 0.5862 mL | 1.1724 mL | 2.9310 mL | |
| 25 mM | 0.0938 mL | 0.4690 mL | 0.9379 mL | 2.3448 mL | |
| 30 mM | 0.0782 mL | 0.3908 mL | 0.7816 mL | 1.9540 mL | |
| 40 mM | 0.0586 mL | 0.2931 mL | 0.5862 mL | 1.4655 mL | |
| 50 mM | 0.0469 mL | 0.2345 mL | 0.4690 mL | 1.1724 mL | |
| 60 mM | 0.0391 mL | 0.1954 mL | 0.3908 mL | 0.9770 mL | |
| 80 mM | 0.0293 mL | 0.1466 mL | 0.2931 mL | 0.7328 mL | |
| 100 mM | 0.0234 mL | 0.1172 mL | 0.2345 mL | 0.5862 mL |
STING agonist-45 Related Classifications
HY-177338 Related Classifications
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