EN1441
Based on 1 Customer Validation
EN1441 is a covalent degrader targeting the androgen receptor (AR) with an EC50 value of 4.2 μM and its truncated variant AR-V7. EN1441 selectively and potently degrades both AR and AR-V7 in androgen-independent prostate cancer cells. EN1441 is promising for research of androgen-independent prostate cancers.
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- 純度: 99.67%
- CAS 番号: 2196448-47-0
- 分子式: C13H13ClN2O2
- 分子量:264.71
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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
生物活性
EN1441 (0.1-50 μM; 1-24 h) shows dose-responsive degradation of AR and AR-V7 with rapid loss occurring at one hour[1].
EN1441 (0.1-100 μM) EN1441 completely inhibits total AR transcriptional activity in androgen-independent prostate cancer cells expressing both AR and AR-V7[1].
EN1441 selectively degrades AR and AR-V7 in a proteasome-dependent manner through direct covalent targeting of an intrinsically disordered cysteine C125 in AR and AR-V7. EN1441 causes significant and selective destabilization of AR and AR-V7, leading to aggregation of AR/AR-V7 and subsequent proteasome-mediated degradation[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:22Rv1 cells
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Concentration:0.1 μM, 1 μM, 10 μM, 50 μM
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Incubation Time:1 h, 3 h, 6 h, 9 h, 12 h, 24 h
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Result:Showed dose-responsive degradation of AR and AR-V7 with rapid loss occurring at one hour.
化学情報
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CAS 番号 2196448-47-0
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性状 Solid
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分子量 264.71
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分子式 C13H13ClN2O2
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Color White to off-white
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SMILES
ClC1=CC2=C(NC(C(N2C(C=C)=O)(C)C)=O)C=C1
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
溶剤 & 溶解度
DMSO : 125 mg/mL (472.21 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. 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. 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 (274 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (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. 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 | 3.7777 mL | 18.8886 mL | 37.7772 mL | 94.4430 mL |
| 5 mM | 0.7555 mL | 3.7777 mL | 7.5554 mL | 18.8886 mL | |
| 10 mM | 0.3778 mL | 1.8889 mL | 3.7777 mL | 9.4443 mL | |
| 15 mM | 0.2518 mL | 1.2592 mL | 2.5185 mL | 6.2962 mL | |
| 20 mM | 0.1889 mL | 0.9444 mL | 1.8889 mL | 4.7221 mL | |
| 25 mM | 0.1511 mL | 0.7555 mL | 1.5111 mL | 3.7777 mL | |
| 30 mM | 0.1259 mL | 0.6296 mL | 1.2592 mL | 3.1481 mL | |
| 40 mM | 0.0944 mL | 0.4722 mL | 0.9444 mL | 2.3611 mL | |
| 50 mM | 0.0756 mL | 0.3778 mL | 0.7555 mL | 1.8889 mL | |
| 60 mM | 0.0630 mL | 0.3148 mL | 0.6296 mL | 1.5740 mL | |
| 80 mM | 0.0472 mL | 0.2361 mL | 0.4722 mL | 1.1805 mL | |
| 100 mM | 0.0378 mL | 0.1889 mL | 0.3778 mL | 0.9444 mL |
EN1441 関連分類
HY-173626 関連分類
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