Apalutamide-13C,d3(Synonyms: ARN-509-13C,d3)

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Apalutamide-13C,d3 (Synonyms: ARN-509-13C,d3)

Apalutamide-13C,d3 是一种 13C- 和氘代标记的 Apalutamide。Apalutamide (ARN-509) 是有效,竞争性的雄激素受体 (AR) 拮抗剂,IC50 为 16 nM

Apalutamide-13C,d3(Synonyms: ARN-509-13C,d3)

Apalutamide-13C,d3 Chemical Structure

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生物活性

Apalutamide-13C,d3 is the 13C- and deuterium labeled. Apalutamide (ARN-509) is a potent and competitive androgen receptor (AR) antagonist, binding AR with an IC50 of 16 nM[1].

体外研究
(In Vitro)

Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs[38].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

481.45

Formula

C2013CH12D3F4N5O2S

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

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

参考文献
  • [1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-223.

    [2]. Clegg NJ, et al. ARN-509: a novel antiandrogen for prostate cancer treatment. Cancer Res. 2012 Mar 15;72(6):1494-503.

    [3]. Smith MR, et al. 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 May 6. pii: S0302-2838(16)30133

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