STING agonist-46
Based on 1 Customer Validation
STING agonist-46 is an orally active STING agonist. STING agonist-46 activates the STING signaling pathway, promoting phosphorylation of TBK1 and IRF3, and secretion of IFN-β and IP-10. STING agonist-46 directly binds to STING and increases its thermal stability. STING agonist-46 demonstrates potent anti-tumor efficacy in B16F10, CT26, and 4T1 mouse models. STING agonist-46 can be used for cancer immunotherapy studies.
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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 98.63%
- CAS 番号: 3033532-05-4
- 分子式: C17H21NO5S
- 分子量:351.42
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保管条件: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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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
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生物活性
STING agonist-46 (Compound 57) (0.37-30 μM, 24 h) exhibits potent activation on ISG pathway in THP1-Dual cells, with EC50 of 2.55 μM[1].
STING agonist-46 (10-50 μM, 24 h) shows potent activation on h-STING in THP1-Blue-ISG cells and m-STING in RAW-Lucia cells[1].
STING agonist-46 (3.3-30 μM, 2 h) significantly promotes phosphorylation of TBK1 and IRF3 in THP1-Dual cells[1].
STING agonist-46 (1.1-30 μM, 24 h) upregulates the expression of IFN-β and IP-10 in THP1-Dual cells[1].
STING agonist-46 (3.3-30 μM, 48 h) activates both hSTING-R232 and hSTING-H232 subtypes in 293T-Dual reporter cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:THP1-Dual cells
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Concentration:1.1, 3.3, 10, 30 μM
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Incubation Time:24 h
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Result:Upregulated the expression of IFN-β and IP-10 in THP1-Dual cells.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:B16F10 melanoma cells (0.5 × 105 in PBS)/CT26 colon tumor cells (2.5 × 105 in PBS)/4T1 breast cancer cells were subcutaneously implanted into the right axilla of 6-week-old female immunocompetent WT C57BL/6 mice or STING-knockout C57BL/6 mice[1]
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Dosage:500 μg/mouse, intratumoral injection or 100 mg/kg, p.o.
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Administration:On days 1, 4, 7
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Result:Demonstrated significant anti-tumor efficacy against B16F10/CT26/4T1 melanoma in immunocompetent mice.
Showed no anti-tumor efficacy against B16F10/CT26 melanoma in STING-knockout mice.
Showed no significant changes in body weight.
化学情報
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CAS 番号 3033532-05-4
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性状 Solid
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分子量 351.42
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分子式 C17H21NO5S
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Color White to light yellow
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SMILES
O=C(CCC(ONC(C)C)=O)C1=CC2=CC(OC)=C(C=C2S1)OC
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
溶剤 & 溶解度
DMSO : 100 mg/mL (284.56 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.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
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: ≥ 5 mg/mL (14.23 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 5 mg/mL (14.23 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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.
純度とドキュメンテーション
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データシート (273 KB)
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取扱説明書 (2659 KB)
参考文献
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 | 2.8456 mL | 14.2280 mL | 28.4560 mL | 71.1399 mL |
| 5 mM | 0.5691 mL | 2.8456 mL | 5.6912 mL | 14.2280 mL | |
| 10 mM | 0.2846 mL | 1.4228 mL | 2.8456 mL | 7.1140 mL | |
| 15 mM | 0.1897 mL | 0.9485 mL | 1.8971 mL | 4.7427 mL | |
| 20 mM | 0.1423 mL | 0.7114 mL | 1.4228 mL | 3.5570 mL | |
| 25 mM | 0.1138 mL | 0.5691 mL | 1.1382 mL | 2.8456 mL | |
| 30 mM | 0.0949 mL | 0.4743 mL | 0.9485 mL | 2.3713 mL | |
| 40 mM | 0.0711 mL | 0.3557 mL | 0.7114 mL | 1.7785 mL | |
| 50 mM | 0.0569 mL | 0.2846 mL | 0.5691 mL | 1.4228 mL | |
| 60 mM | 0.0474 mL | 0.2371 mL | 0.4743 mL | 1.1857 mL | |
| 80 mM | 0.0356 mL | 0.1778 mL | 0.3557 mL | 0.8892 mL | |
| 100 mM | 0.0285 mL | 0.1423 mL | 0.2846 mL | 0.7114 mL |
STING agonist-46 関連分類
HY-175714 関連分類
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