Apalutamide (ARN-509)是一种有效且竞争性的雄激素受体 (AR) 拮抗剂,具有高亲和力,可用于前列腺癌等相关研究。
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英文别名 (English Synonym) |
ARN-509 |
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中文名称 (Chinese Name) |
达比加群酯 |
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靶点 (Target) |
Androgen Receptor |
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通路 (Pathway) |
Endocrinology and Hormones |
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CAS号 (CAS NO.) |
956104-40-8 |
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分子式 (Formula) |
C21H15F4N5O2S |
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分子量 (Molecular Weight) |
477.43 |
|
纯度 (Purity) |
≥98% |
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溶解性 (Solubility) |
溶于DMSO |
-25~-15℃保存,有效期3年
[1] Smith MR, Antonarakis ES, Ryan CJ, Berry WR, Shore ND, Liu G, Alumkal JJ, Higano CS, Chow Maneval E, Bandekar R, de Boer CJ, Yu MK, Rathkopf DE. Phase 2 Study of the Safety and Antitumor Activity of Apalutamide (ARN-509), a Potent Androgen Receptor Antagonist, in the High-risk Nonmetastatic Castration-resistant Prostate Cancer Cohort. Eur Urol. 2016 Dec,70(6):963-970. doi: 10.1016/j.eururo.2016.04.023. Epub 2016 May 6. PMID: 27160947, PMCID: PMC5568792.[2]Clegg NJ, Wongvipat J, Joseph JD, Tran C, Ouk S, Dilhas A, Chen Y, Grillot K, Bischoff ED, Cai L, Aparicio A, Dorow S, Arora V, Shao G, Qian J, Zhao H, Yang G, Cao C, Sensintaffar J, Wasielewska T, Herbert MR, Bonnefous C, Darimont B, Scher HI, Smith-Jones P, Klang M, Smith ND, De Stanchina E, Wu N, Ouerfelli O, Rix PJ, Heyman RA, Jung ME, Sawyers CL, Hager JH. ARN-509: a novel antiandrogen for prostate cancer treatment. Cancer Res. 2012 Mar 15,72(6):1494-503. doi: 10.1158/0008-5472.CAN-11-3948. Epub 2012 Jan 20. PMID: 22266222, PMCID: PMC3306502.





