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Androgen receptor antagonist 1

Catalog No. T10320 CAS 1338812-36-4

Androgen receptor antagonist 1 is an orally available full androgen receptor antagonist (IC50: 59 nM). It can be used in the synthesis of PROTAC AR degraders, which results in 24% and 47 % AR protein degradation in LNCaP cells at 1 μM and 10 μM, respectively.

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Androgen receptor antagonist 1 Chemical Structure

Androgen receptor antagonist 1, CAS 1338812-36-4

Pack Size	Availability	Price/USD
25 mg	6-8 weeks	$ 1,520.00
50 mg	6-8 weeks	$ 1,980.00
100 mg	6-8 weeks	$ 2,500.00

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This compound is a customized synthesis product. We have a strong synthesis team with excellent synthesis technology and capabilities. However, due to various objective factors, there is a low probability that the synthesis will not be successful. If you need to learn more, please feel free to consult us, we will serve you wholeheartedly.

Biological Description

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Description	Androgen receptor antagonist 1 is an orally available full androgen receptor antagonist (IC50: 59 nM). It can be used in the synthesis of PROTAC AR degraders, which results in 24% and 47 % AR protein degradation in LNCaP cells at 1 μM and 10 μM, respectively.
Targets&IC50	Androgen receptor:59 nM
In vitro	Androgen receptor antagonist 1 (Compound 26; 1 nM-100 μM) shows significant cell growth inhibition effects for LNAR and LNCaP cells but not DU145 cells [1].
In vivo	Androgen receptor antagonist 1 (100 mg/kg once a day for 5 weeks) shows excellent in vivo tumor growth inhibition upon oral administration in castration-resistant prostate cancer (CRPC) animal model [1].

Molecular Weight	416.9
Formula	C21H25ClN4O3
CAS No.	1338812-36-4

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

References and Literature

1. Guo C, et al. Discovery of aryloxy tetramethylcyclobutanes as novel androgen receptor antagonists. J Med Chem. 2011 Nov 10;54(21):7693-704. 2. Han X, et al. Discovery of ARD-69 as a Highly Potent Proteolysis Targeting Chimera (PROTAC) Degrader of Androgen Receptor (AR) for the Treatment of Prostate Cancer. J Med Chem. 2019 Jan 24;62(2):941-964.

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Androgen receptor antagonist 1 1338812-36-4 Others inhibitor inhibit

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