SNX281
Based on 1 Customer Validation
SNX281 is a selective STING agonist, with IC50 values of 4.1, 4.5, 10.7, and 3.7 μM against human, mouse, rat, and monkey STING, respectively. SNX281 undergoes homodimerization at the STING binding site, triggering a conformational shift of STING from an inactive open state to an active closed state, thereby driving downstream STING-dependent signaling pathways. SNX281 induces type I interferons, IFN-β, TNF-α, IL-6, cytokine release, T cell responses, and long-lasting immune memory. SNX281 exhibits anti-tumor activity and is applicable to research related to colorectal cancer, melanoma, advanced solid tumors, lymphoma, and ovarian cancer.
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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: 98.96%
- CAS 番号: 2332803-84-4
- 分子式: C20H20ClNO3S
- 分子量:389.90
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保管条件:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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
SNX281 (25 µM; 1 h) induces STING translocation, TBK1 phosphorylation, and IRF3 nuclear translocation in HEK293T cells stably expressing human HAQ-mutant STING[1].
SNX281 (10 µM; 0-2 h) rapidly induces the phosphorylation of STING, TBK1 and IRF3 in THP-1 cells[1].
SNX281 (6 h) induces dose-dependent secretion of IFN-β, TNF-α and IL-6 in THP-1 cells[1].
SNX281 induces IRF3 and NF-κB reporter gene activity in a STING-dependent manner in THP1-Dual cells, with an EC50 value of 1.1 µM for human wild-type STING and 1.7 µM for human HAQ mutant STING[1].
SNX281 (6 h) induces dose-dependent IFN-β secretion in J774A.1 mouse macrophage-like cells, with an EC50 of 5.4 µM[1].
SNX281 (6 h) induces dose-dependent IFN-β secretion in peripheral blood mononuclear cells of cynomolgus monkeys, with an EC50 of 2.4 µM[1].
SNX281 induces STING-dependent pathway activation in THP-1 cells and human peripheral blood mononuclear cells (PBMCs), and promotes the production of IFN-β, TNF-α and IL-6[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:THP-1 cells
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Concentration:/
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Incubation Time:6 hours
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Result:Induced dose-dependent secretion of IFN-β with an EC50 of 6.6 µM.
Induced dose-dependent secretion of TNF-α with an EC50 of 7.9 µM.
Induced dose-dependent secretion of IL-6 with an EC50 of 5.5 µM.
| Species | Dose | Route | T1/2 | AUC0-∞ | Vss | CL |
|---|---|---|---|---|---|---|
| Mice[1] | 5 mg/kg | i.v. | 2.33 h | 16766 ng·h/mL | 0.984 L/kg | 4.97 mL/min/kg |
SNX281 (12.5-45 mg/kg; intravenous administration) exhibits dose-dependent antitumor activity in the BALB/c CT26 colorectal cancer 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 (male/female)[1]
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Dosage:10 mg/kg; 25 mg/kg; 35 mg/kg; 45 mg/kg
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Administration:i.v.; single bolus
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Result:Induced dose-dependent elevated plasma IFN-β levels at 3 hours post-dose, with levels highest at 3 hours, reduced at 6 hours, and undetectable by 24 hours across all doses.
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Animal Model:BALB/c ( colorectal cancer model via subcutaneous inoculation of CT26.WT cells)[1]
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Dosage:12.5 mg/kg (Days 1/4/7 dosing); 25 mg/kg (Days 1/4/7 dosing); 25 mg/kg (b.i.d. on Day 1); 35 mg/kg (single dose); 45 mg/kg (single dose)
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Administration:i.v.; single doses on Days 1, 4, 7; i.v.; two doses 2 hours apart on Day 1; i.v.; single bolus on Day 1
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Result:Yielded 0/8 complete responses (CRs) at 12.5 mg/kg (Days 1/4/7).
Yielded 1/8 CRs at 25 mg/kg (Days 1/4/7).
Yielded 3/8 CRs at 25 mg/kg (b.i.d.
on Day 1).
Yielded 8/8 CRs (complete tumor regression in all mice) at 35 mg/kg (single dose).
Yielded 8/8 CRs (complete tumor regression in all mice) at 45 mg/kg (single dose).
Increased circulating CD8+ T cells by ~2-fold at 35 mg/kg or 45 mg/kg single doses compared to vehicle controls.
Caused no significant body weight loss across all treatment groups.
化学情報
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CAS 番号 2332803-84-4
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性状 Solid
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分子量 389.90
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分子式 C20H20ClNO3S
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Color Off-white to light yellow
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SMILES
O=C(CN1C2=CC(C(C)(C)C)=CC=C2C(C3=CC=C(C(SC)=C31)Cl)=O)O
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
溶剤 & 溶解度
DMSO : 15 mg/mL (38.47 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 (protect from light). 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 (protect from light). 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)
純度とドキュメンテーション
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データシート (280 KB)
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SDS (251 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 (protect from light). 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 | 2.5648 mL | 12.8238 mL | 25.6476 mL | 64.1190 mL |
| 5 mM | 0.5130 mL | 2.5648 mL | 5.1295 mL | 12.8238 mL | |
| 10 mM | 0.2565 mL | 1.2824 mL | 2.5648 mL | 6.4119 mL | |
| 15 mM | 0.1710 mL | 0.8549 mL | 1.7098 mL | 4.2746 mL | |
| 20 mM | 0.1282 mL | 0.6412 mL | 1.2824 mL | 3.2060 mL | |
| 25 mM | 0.1026 mL | 0.5130 mL | 1.0259 mL | 2.5648 mL | |
| 30 mM | 0.0855 mL | 0.4275 mL | 0.8549 mL | 2.1373 mL |
SNX281 関連分類
HY-160406 関連分類
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