YS3375
YS3375 is an ENPP1 inhibitor with an IC50 of 19.4 nM. YS3375 prevents cGAMP hydrolysis and sustains STING pathway activation. YS3375 can be used for research on colorectal cancer.
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: C23H22F3N4O4P
- 分子量:506.41
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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
- 参考文献
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Help & FAQs
生物活性
製品説明
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| MDA-MB-231 | IC50 |
186 nM
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Inhibition of intracellular ENPP1 in human MDA-MB-231 breast cancer cells using thymidine-5′-monophosphate p-nitrophenyl ester as substrate after 10 min compound preincubation and 60 min reaction measuring p-nitrophenol absorbance at 405 nm.
Inhibition of intracellular ENPP1 in human MDA-MB-231 breast cancer cells using thymidine-5′-monophosphate p-nitrophenyl ester as substrate after 10 min compound preincubation and 60 min reaction measuring p-nitrophenol absorbance at 405 nm.
|
42648057 |
| CHO-K1 | IC50 |
30 μM
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Inhibition of hERG current in CHO-K1 cells transfected with hERG by whole-cell patch clamp with IC50 >30 μM.
Inhibition of hERG current in CHO-K1 cells transfected with hERG by whole-cell patch clamp with IC50 >30 μM.
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42648057 |
体外実験
YS3375 (pre-incubation for 10 min; substrate reaction for 60 min) inhibits cell-associated ENPP1 in MDA-MB-231 cells with an IC50 of 186 nM[1].
YS3375 (24 h) showed no obvious cytotoxicity in THP-1, THP1-Blue ISG, or THP1-Dual KO-STING cells within 24 h[1].
YS3375 (1-30 μM) showed weak inhibition of hERG current in CHO-K1 cells, with an IC50 >30 μM[1].
YS3375 exhibited the poorest stability in monkey liver microsomes (t1/2 24.1 min)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:THP-1, THP1-Blue ISG, and THP1-Dual KO-STING cells
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Concentration:serial dilutions
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Incubation Time:24 h
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Result:Showed no obvious cytotoxicity within the tested concentration range.
体内実験
YS3375 (40 mg/kg; intraperitoneal; daily) combined with anti-PD-1 (intraperitoneal; every other day) produces 67% TGI in the CT-26 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:BALB/c (female, 6 to 8 weeks of age)[1]
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Dosage:40 mg/kg
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Administration:intraperitoneal; daily
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Result:Achieved a tumor growth inhibition rate of 50% at 40 mg/kg in the CT-26 colorectal cancer model.
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Animal Model:BALB/c (female, 6 to 8 weeks of age)[1]
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Dosage:40 mg/kg (YS3375); anti-PD-1 antibody
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Administration:YS3375 intraperitoneal; daily; anti-PD-1 antibody intraperitoneal; every other day
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Result:In combination with anti-PD-1 antibody, YS3375 at 40 mg/kg achieved a tumor growth inhibition rate of 67% in the CT-26 colorectal cancer model.
化学情報
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分子量 506.41
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分子式 C23H22F3N4O4P
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SMILES
FC(C=CC=C1F)=C1C2=NC(C(NC3=CC(F)=CC=C3N4CCC(CP(O)(O)=O)CC4)=O)=CN=C2
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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)
YS3375 関連分類
HY-189633 関連分類
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