MSA-2-Pt
MSA-2-Pt, platinum salt-modified MSA-2 (HY-136927), is a STING agonist. MSA-2-Pt inducing cell
death by platinum and activating the STING pathway by MSA-2. MSA-2-Pt direct activates STING pathway, induces phosphorylation of TBK1, IRF3, and NF-κB p65. MSA-2-Pt enhances tumor infiltration of CD4+ and CD8+ T cells, and induces tumor cell death and apoptosis in mouse colon carcinoma and melanoma models.
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- CAS 番号: 3028778-96-0
- 分子式: C28H32N2O10PtS2
- 分子量:815.78
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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
- 純度とドキュメンテーション
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Help & FAQs
生物活性
death by platinum and activating the STING pathway by MSA-2. MSA-2-Pt direct activates STING pathway, induces phosphorylation of TBK1, IRF3, and NF-κB p65. MSA-2-Pt enhances tumor infiltration of CD4+ and CD8+ T cells, and induces tumor cell death and apoptosis in mouse colon carcinoma and melanoma models[1].
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TBK1 |
IRF3 |
MSA-2-Pt (25-300 μM; 12-24 h) induces dose-dependent cell death in mouse colon adenocarcinoma MC38 cells, with significant cytotoxicity observed at concentrations ≥75 μM after 24 h[1].
MSA-2-Pt (10-50 μM; 24 h) activates IFN-β secretion in mouse macrophage RAW264.7 cells[1].
MSA-2-Pt (10-50 μM; 3 h) activates the STING signaling pathway in mouse macrophage RAW264.7 cells, inducing phosphorylation of STING, TBK1, IRF3, and NF-κB p65 at concentrations of 10, 25, and 50 μM after 3 h[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:mouse colon adenocarcinoma MC38 cells
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Concentration:25 μM, 50 μM, 75 μM, 100 μM, 200 μM, 300 μM
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Incubation Time:12; 24 h;
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Result:Induced significant MC38 cell death starting at 75 μM, with a dose-dependent reduction in cell viability.
Reduced cell viability to ~20% or lower at 100 μM and above.
Confirmed significant pyroptotic cell death in MC38 cells treated with 75 μM for 12 h and 24 h via microscopic imaging.
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Cell Line:mouse macrophage RAW264.7 cells
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Concentration:10 μM, 25 μM, 50 μM
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Incubation Time:3 h
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Result:Increased levels of phosphorylated P65 (p-P65) compared to control.
Induced phosphorylation of STING, TBK1, and IRF3 in a concentration-dependent manner.
MSA-2-Pt (150 μg; i.t.; three doses on day 9, 11, 15) exhibits significant antitumor efficacy in poorly immunogenic B16F10 melanoma-bearing mice, with 22% of treated mice achieving tumor-free status and significantly extended survival[1].
MSA-2-Pt (150 μg; i.t.; single dose) activates the STING pathway (via elevated serum IFN-β), enhances tumor infiltration of CD4+ and CD8+ T cells, and induces tumor cell death and apoptosis in MC38 colon carcinoma-bearing mice[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Colon carcinoma C57BL/6 mice (female, 6 weeks old, subcutaneous injection of 2×105 MC38 cells)[1]
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Dosage:150 μg
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Administration:intratumorly injection; three doses on day 13, 15, 19
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Result:Significantly reduced tumor growth relative to the control group.
Achieved tumor-free status in 7 out of 9 treated mice.
Significantly increased survival compared to the control group.
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Animal Model:Melanoma C57BL/6 mice (female, 6 weeks old, subcutaneous injection of 2×105 B16F10 cells)[1]
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Dosage:150 μg
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Administration:intratumorly injection; three doses
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Result:Significantly reduced tumor growth relative to the control group.
Achieved tumor-free status in 2 out of 9 treated mice.
Significantly increased survival compared to the control group.
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Animal Model:Colon carcinoma C57BL/6 mice (female, 6 weeks old, subcutaneous injection of 2×105 MC38 cells)[1]
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Dosage:150 μg
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Administration:intratumorly injection; single dose
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Result:Increased serum IFN-β levels significantly relative to the control group.
Increased the ratio of CD4+ T cells of total cells and CD8+ T cells of total cells in tumor tissue relative to the control group.
Induced significant tumor cell death observed via H&E staining.
Induced a significantly higher proportion of tumor cell apoptosis observed via TUNEL staining.
化学情報
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CAS 番号 3028778-96-0
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分子量 815.78
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分子式 C28H32N2O10PtS2
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SMILES
O=C(CCC(C1=CC2=C(C=C(C(OC)=C2)OC)S1)=O)[O-][Pt+2]([NH3])([NH3])[O-]C(CCC(C3=CC4=C(C=C(C(OC)=C4)OC)S3)=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
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
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参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
MSA-2-Pt 関連分類
HY-162133 関連分類
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