5N-Bicalutamide
5N-Bicalutamide is an androgen receptor (AR) antagonist with a Ki of 0.15 nM. 5N-Bicalutamide is a derivative of Bicalutamide (HY-14249). 5N-Bicalutamide reacts with Cys784 in the AR binding pocket via an activated aryl nitrile group to form a reversible thioimidate covalent adduct, which significantly enhances its binding affinity and inhibitory potency. 5N-Bicalutamide is used in prostate cancer-related research.
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- No. CAS: 1845688-96-1
- Fòrmula: C17H13F4N3O4S
- Peso molecular:431.36
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Actividad biológica
Descripciòn
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HeLa | IC50 |
0.015 μM
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Inhibition of DHT-induced androgen receptor transactivation in HeLa cells expressing AR-LBD fused to Gal4-DBD, assessed via luciferase reporter assay after overnight incubation with 1 nM DHT.
Inhibition of DHT-induced androgen receptor transactivation in HeLa cells expressing AR-LBD fused to Gal4-DBD, assessed via luciferase reporter assay after overnight incubation with 1 nM DHT.
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28981251 |
In Vitro
5N-Bicalutamide (100 μM; 1-24 h) reacts rapidly with free cysteine in physiological buffer, forming a thiazoline adduct with 99% conversion after 4 h at 37 °C, pH 7.4[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:LNCaP/AR and HeLa cells
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Concentration:3 μM, 10 μM, 30 μM
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Incubation Time:24 h
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Result:Produced no significant cytotoxicity.
Chemical Information
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No. CAS 1845688-96-1
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Peso molecular 431.36
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Fòrmula C17H13F4N3O4S
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SMILES
N#CC1=NC=C(C=C1C(F)(F)F)NC(=O)C(O)(C)CS(=O)(=O)C2=CC=C(F)C=C2
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
5N-Bicalutamide Related Classifications
HY-125589 Related Classifications
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