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Art. -Nr.: HY-125589

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5N-Bicalutamide

5N-Bicalutamide is an androgen receptor (AR) antagonist with a K_i 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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CAS. Nr.: 1845688-96-1
Formel: C₁₇H₁₃F₄N₃O₄S
Molecular Weight:431.36

Speicherung:

Please store the product under the recommended conditions in the Certificate of Analysis.

5N-Bicalutamide Chemical Structure

CAS. Nr.: 1845688-96-1

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Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- Cellular Effect
- In Vitro
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
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Biologische Aktivität

Beschreibung

Cellular Effect

Cell Line	Type	Value	Description	References
HeLa	IC50	0.015 μM	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.	28981251

In Vitro

5N-Bicalutamide has a 10-fold higher electrophilicity than bicalutamide, as measured by the calculated free energy of thioimidate formation with methanethiol^[1].
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.

Cell Cytotoxicity Assay^[1]

Cell Line:

LNCaP/AR and HeLa cells
Concentration:

3 μM, 10 μM, 30 μM
Incubation Time:

24 h
Result:

Produced no significant cytotoxicity.

Chemical Information

CAS. Nr. 1845688-96-1
Molecular Weight 431.36
Formel C₁₇H₁₃F₄N₃O₄S
SMILES

N#CC1=NC=C(C=C1C(F)(F)F)NC(=O)C(O)(C)CS(=O)(=O)C2=CC=C(F)C=C2
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

Please store the product under the recommended conditions in the Certificate of Analysis.

Reinheit & Dokumentation

Handling Instructions (2659 KB)

Verweise

[1]. de Jesus Cortez F, et al. Development of 5N-Bicalutamide, a High-Affinity Reversible Covalent Antiandrogen. ACS chemical biology. 2017 Dec 15;12(12):2934-2939.

Calculators

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Bioz

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MOQ

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100 mg

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