Apalutamide (ARN-509) | AR antagonist | Probechem Biochemicals

Chemical Structure : Apalutamide

CAS No.: 956104-40-8

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Apalutamide (ARN-509, ARN509, JNJ 56021927)

货号: PC-73182Not For Human Use, Lab Use Only.

Apalutamide (ARN-509) is a potent and competitive androgen receptor (AR) antagonist with binding IC50 of 16 nM.

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5 mg	￥780	In stock
10 mg	￥1180	In stock
50 mg	￥2480	In stock
100 mg	￥3780	In stock
250 mg		Get quote

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生物&药学活性

Apalutamide (ARN-509) is a potent and competitive androgen receptor (AR) antagonist with binding IC50 of 16 nM.
Apalutamide (ARN-509) targets the AR ligand-binding domain and prevents AR nuclear translocation, DNA binding, and transcription of AR gene targets, inhibits AR transcriptional activity and prostate cancer cell proliferation.
ARN-509 lacked significant agonist activity in preclinical models of CRPC compared to bicalutamide.
ARN-509 showed greater efficacy than MDV3100 in a clinically valid murine xenograft model of human CRPC.

物理化学性质&存储条件

分子量	477.43
分子式	C21H15F4N5O2S
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	4-(7-(6-Cyano-5-(trifluoromethyl)pyridin-3-yl)-8-oxo-6-thioxo-5,7-diazaspiro[3.4]octan-5-yl)-2-fluoro-N-methylbenzamide

参考文献

1. Joseph JD, et al. Cancer Discov. 2013 Sep;3(9):1020-9.

2. Clegg NJ, et al. Cancer Res. 2012 Mar 15;72(6):1494-503.

Apalutamide (ARN-509, ARN509, JNJ 56021927)

生物&药学活性

物理化学性质&存储条件

参考文献

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Apalutamide (ARN-509, ARN509, JNJ 56021927)

生物&药学活性

物理化学性质&存储条件

参考文献

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