S2157
Based on 1 Customer Validation
S2157, a N-alkylated tranylcypromine (TCP) derivative, is a potent lysine-specific demethylase 1 (LSD1) inhibitor. S2157 increases H3K9 methylation and reciprocal H3K27 deacetylation at super-enhancer regions. S2157 induces apoptosis in TCP-resistant T-cell acute lymphoblastic leukemia (T-ALL) cells by repressing transcription of the NOTCH3 and TAL1 genes. S2157 efficiently pass through the blood-brain barrier and can almost completely eradicate CNS leukemia in mice transplanted with T-ALL cells.
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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: 98.44%
- CAS 番号: 2262488-39-9
- 分子式: C23H28ClF2N3O2
- 分子量:451.94
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保管条件:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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
LSD1[1]
S2157 is particularly effective for T-ALL cell lines with the IC50 values between 1.1 µM for human T-ALL cell lines CEM and 6.8 µM for MOLT4[1].
S2157 (4-20 µM; 72 hours) modestly inhibits mitogen-activated normal T-lymphocytes[1].
S2157 (4-8 µM; 24 hours) induces apoptosis and down-regulates the expression of NOTCH3 and TAL1 proteins in T-cell acute lymphoblastic leukemia (T-ALL) cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Normal T-lymphocytes
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Concentration:4, 8, 12, 16, 20 µM
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Incubation Time:For 72 hours
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Result:Modestly inhibited mitogen-activated normal T-lymphocytes.
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Cell Line:T-cell acute lymphoblastic leukemia (T-ALL) cells
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Concentration:4, 6, 8 µM
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Incubation Time:For 24 hours
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Result:Induced apoptosis, as evidenced by increased annexin-V reactivity on flow cytometry in T-ALL cells in a dose- and time-dependent manner without affecting cell cycle distribution.
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Cell Line:T-ALL cells
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Concentration:4, 6, 8 µM
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Incubation Time:For 24 hours
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Result:Down-regulated the expression of NOTCH3 and TAL1 proteins in T-ALL cells.
S2157 (50 mg/kg; IP) has a T1/2 of 0.88 hours, a Cmax of 4.33 μM and an AUC of 5.75 μM•h[1].
S2157 (30 mg/kg or 50 mg/kg; twice a week for 3 weeks) almost completely suppressed the growth of MOLT4 cells in most but not all NOD/SCID mice with MOLT4 cells. S2157 eradicates CNS leukemia in murine xenotransplanted models[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Nonobese diabetic/severe combined immunodeficiency (NOD/SCID) mice with MOLT4 cells[1]
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Dosage:50 mg/kg
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Administration:IP; 3 times a week; for 28 days
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Result:The size of subcutaneous tumors reduced to less than 20% of that in the untreated control.
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Animal Model:8-week-old ICR mice[1]
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Dosage:50 mg/kg (Pharmacokinetic Analysis)
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Administration:IP
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Result:Had a T1/2 of 0.88 hours, a Cmax of 4.33 μM and an AUC of 5.75 μM•h.
化学情報
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CAS 番号 2262488-39-9
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性状 Solid
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分子量 451.94
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分子式 C23H28ClF2N3O2
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Color White to off-white
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SMILES
[H]Cl.CN1CCN(C(CN[C@H]2[C@H](C3=CC(F)=CC(F)=C3OCC4=CC=CC=C4)C2)=O)CC1.[Relative stereochemistry]
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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, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
溶剤 & 溶解度
DMSO : 100 mg/mL (221.27 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 (sealed storage, away from moisture). 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 (sealed storage, away from moisture). 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 (282 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 (sealed storage, away from moisture). 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 | 2.2127 mL | 11.0634 mL | 22.1268 mL | 55.3171 mL |
| 5 mM | 0.4425 mL | 2.2127 mL | 4.4254 mL | 11.0634 mL | |
| 10 mM | 0.2213 mL | 1.1063 mL | 2.2127 mL | 5.5317 mL | |
| 15 mM | 0.1475 mL | 0.7376 mL | 1.4751 mL | 3.6878 mL | |
| 20 mM | 0.1106 mL | 0.5532 mL | 1.1063 mL | 2.7659 mL | |
| 25 mM | 0.0885 mL | 0.4425 mL | 0.8851 mL | 2.2127 mL | |
| 30 mM | 0.0738 mL | 0.3688 mL | 0.7376 mL | 1.8439 mL | |
| 40 mM | 0.0553 mL | 0.2766 mL | 0.5532 mL | 1.3829 mL | |
| 50 mM | 0.0443 mL | 0.2213 mL | 0.4425 mL | 1.1063 mL | |
| 60 mM | 0.0369 mL | 0.1844 mL | 0.3688 mL | 0.9220 mL | |
| 80 mM | 0.0277 mL | 0.1383 mL | 0.2766 mL | 0.6915 mL | |
| 100 mM | 0.0221 mL | 0.1106 mL | 0.2213 mL | 0.5532 mL |
S2157 関連分類
HY-136523 関連分類
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