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.
For research use only. We do not sell to patients.
- Purity: 99.67%
- CAS No.: 2196448-47-0
- Formula: C13H13ClN2O2
- Molecular Weight:264.71
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Anti-Cancer Compound Library
HY-L025
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Transcription Factor-Targeted Library
HY-L090
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Anti-Prostate Cancer Compound Library
HY-L124
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Nuclear Receptor Compound Library
HY-L126
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Bioactive Compound Library Max
HY-L181
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MCE Bioactive Compound Library
HY-L001V
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Bioactive Compound Library
HY-L001
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High-Throughput Bioactive Compound Library
HY-L205
Biological Activity
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.
Chemical Information
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CAS No. 2196448-47-0
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Appearance Solid
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Molecular Weight 264.71
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Formula 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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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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Data Sheet (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)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
References
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 |
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