956104-40-8 ARN 509

ARN 509

英文名称:ARN-509
CAS:

956104-40-8

分子式:C21H15F4N5O2S
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ARN 509简介

Apalutamide (INN) (developmental code name ARN-509, also JNJ-56021927) is a non-steroidal antiandrogen that is under development for the treatment of prostate cancer. It is similar to enzalutamide both structurally and pharmacologically, acting as a selective competitive antagonist of the androgen receptor (AR), but shows some advantages, including greater potency and reduced central nervous system permeation. Apalutamide binds weakly to the GABAA receptor similarly to enzalutamide, but due to its relatively lower central concentrations, may have a lower risk of seizures in comparison.
The drug has been found to be effective and well-tolerated in clinical trials thus far, with the most common side effects reported including fatigue, nausea, abdominal pain, and diarrhea.
Apalutamide is currently in phase III clinical trials for castration-resistant prostate cancer.
Recently, the acquired F876L mutation of the AR identified in advanced prostate cancer cells was found to confer resistance to both enzalutamide and apalutamide. A newer antiandrogen, darolutamide (ODM-201), is not affected by this mutation, nor has it been found to be affected by any other tested/well-known AR mutations.; Apalutamide may be effective in a subset of prostate cancer patients with acquired resistance to abiraterone acetate.

ARN 509基本信息

中文名称 ARN 509 英文名称 ARN-509
中文别名

阿帕鲁他胺;

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英文别名

QCR-211; 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; ARN 509; Benzamide,4-[7-[6-cyano-5-(trifluoromethyl)-3-pyridinyl]-8-oxo-6-thioxo-5,7-diazaspiro[3.4]oct-5-yl]-2-fluoro-N-methyl; 4-[7-(6-cyano-5-trifluoromethylpyridin-3-yl)-8-oxo-6-thioxo-5,7-diazaspiro[3.4]oct-5-yl]-2-fluoro-N-methylbenzamide; N-methyl-4-[7-(6-cyano-5-trifluoromethylpyridin-3-yl)-8-oxo-6-thioxo-5,7-diazaspiro[3.4]octan-5-yl]-2-fluorobenzamide; 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; ARN-509; JNJ-56021927; JNJ-927; 4-[7-[6-cyano-5-(trifluoromethyl)pyridin-3-yl]-8-oxo-6-sulfanylidene-5,7-diazaspiro[3.4]octan-5-yl]-2-fluoro-N-methylbenzamide; Erleada ®; A52;

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CAS号 956104-40-8 分子式 C21H15F4N5O2S
分子量 477.43500 精确质量 477.08800
PSA 121.42000 LOGP 4.05248

ARN 509编号系统

MDL号 MFCD28142762
SDS 1.0 中文 展开
SDS 1.0 英文 展开
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核磁图谱 1H NMR : Predict

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ARN 509
CAS号:956104-40-8 分子式:C21H15F4N5O2S 分子量:477.43500

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