N-Desmethyl-Apalutamide

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N-Desmethyl-Apalutamide  纯度: 97.24%

N-Desmethyl Apalutamide 是 Apalutamide 的活性代谢产物，是一种低活性的雄激素受体拮抗剂，其作用力是 Apalutamide 活性的三分之一。N-Desmethyl Apalutamide 的形成主要由 CYP2C8 和 CYP3A4 介导。N-Desmethyl Apalutamide 是中等至强的 CYP3A4 和 CYP2B6 诱导剂，并具有优异的血浆蛋白结合浓度。

N-Desmethyl-Apalutamide

N-Desmethyl-Apalutamide Chemical Structure

CAS No. : 1332391-11-3

规格 价格 是否有货 数量
1 mg ￥2500 In-stock
5 mg ￥5500 In-stock
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N-Desmethyl-Apalutamide 相关产品

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生物活性

N-Desmethyl Apalutamide is an active metabolite of Apalutamide. N-Desmethyl Apalutamide is a less potent antagonist of the androgen receptor and is responsible for one-third of the activity of Apalutamide. The formation of N-Desmethyl Apalutamide mediated predominantly by CYP2C8 and CYP3A4. N-Desmethyl Apalutamide is moderate to strong CYP3A4 and CYP2B6 inducer and has an excellent plasma-proteins bound concentration[1][2][3].

IC50 & Target

CYP3A4 and CYP2B6[1]; Androgen receptor[2]
分子量

463.41

Formula

C20H13F4N5O2S
CAS 号

1332391-11-3
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
参考文献

  • [1]. Pérez-Ruixo C, et al. Population Pharmacokinetics of Apalutamide and its Active Metabolite N-Desmethyl-Apalutamide in Healthy and Castration-Resistant Prostate Cancer Subjects. Clin Pharmacokinet. 2019 Aug 20.

    [2]. 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

    [3]. May MB, et al. Apalutamide: A new agent in the management of prostate cancer. J Oncol Pharm Pract. 2019 Dec;25(8):1968-1978.

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