ZSA-215
ZSA-215 is a potent and orally active STING agonist with an EC50 of 3.3 μM. ZSA-215 enhances STING signaling through promoting the phosphorylation of STING and interferon regulatory factor 3 (IRF3) and secretion of IFN-β. ZSA-215 inhibits tumor regression and long-term survival of mice in MC38 colon cancer model. ZSA-215 can be used to the study of colon cancerr.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
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。
- 分子式: C16H18FNO5Se
- 分子量:402.28
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
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
- プロトコル
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
生物活性
製品説明
体外実験
ZSA-215 (Compound 2dr) (0-1.5 μM, 24 h) displays an EC50 as low as 3.3 μM in THP1-Blue ISG cells[1].
ZSA-215 (0.5-1.5 μM, 24 h) displays best activity for STINGR232 (EC50 = 9.0 μM) and mSTING (EC50 = 9.3 μM) in THP1 cells[1].
ZSA-215 (6-13 μM, 24 h) dramatically induces the expression of IFN-β in THP1 cells[1].
ZSA-215 (13-50 μM, 3 h) significantly increases the phosphorylation of STING and IRF3 in THP1-Blue ISG 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 cells
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Concentration:6 μM, 13 μM
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Incubation Time:24 h
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Result:Enhanced STING signaling through promoting the secretion of IFN-β.
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Cell Line:THP1-Blue ISG cells
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Concentration:13 μM, 25 μM, 50 μM
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Incubation Time:3 h
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Result:Significantly increased the phosphorylation of STING and IRF3.
Parmacokinetics
体内実験
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:MC38 tumor model established in BALB/C female mice (6 weeks)[1]
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Dosage:60 mg/kg
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Administration:Oral administration (p.o.), every 3 Days, 2 or 6 doses
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Result:Achieved CR and long-term survival of all mice, which significantly exceeded its parental compound ZSA-52 (CR = 60%) in combination with anti-PD-1.
Reached CR and long-term survival of all mice with monotherapy.
Did not show any tumor recurrence during additional 74 days observation (total 157 days observation).
Achieved a 60% complete response (CR) rate in mice following two-dose administration.
Produced a high concentration of IFN-β, IL-6 and CXCL10 in tumor and serum, which outperformed MSA-2.
化学情報
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分子量 402.28
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分子式 C16H18FNO5Se
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SMILES
COC1=C(C=C2C([Se]C(C(NC[C@H](C(O)=O)CC)=O)=C2F)=C1)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
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
ZSA-215 関連分類
HY-174308 関連分類
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