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製品番号: 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.

商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
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CAS 番号: 1845688-96-1
分子式: C₁₇H₁₃F₄N₃O₄S
分子量:431.36

保管条件:

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

5N-Bicalutamide 構造式

CAS 番号: 1845688-96-1

価格（税別）

Amount: USD 0.00

* アイテムを追加する前、数量をご選択ください

Use of MCE Products

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

生物活性

製品説明

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

体外実験

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.

化学情報

CAS 番号 1845688-96-1
分子量 431.36
分子式 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
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件

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

純度とドキュメンテーション

取扱説明書 (2659 KB)

参考文献

[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.

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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.

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MOQ

Minimum order quantity

100 mg

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