N-Desmethyl-Apalutamide-15N,d4
N-Desmethyl-Apalutamide-15N,d4 is the 15N and deuterium labeled isotope of N-Desmethyl-Apalutamide (HY-135331). N-Desmethyl-Apalutamide, the major active metabolite of Apalutamide (HY-16060), is a selective competitive inhibitor of androgen receptor. N-Desmethyl-Apalutamide is catalyzed by CYP3A4 and CYP2C8 enzymes. The plasma protein binding rate of N-Desmethyl-Apalutamide reaches 95%, with albumin as the primary binding protein. N-Desmethyl-Apalutamide is suitable for prostate cancer-related research.
For research use only. We do not sell to patients.
- Formula: C20H9D4F4N415NO2S
- Molecular Weight:468.43
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
1. This compound can be used as a tracer
2. This compound can be used as an internal standard for quantitative analysis by NMR, GC-MS, or LC-MS.
Chemical Information
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Unlabeled Cas 1332391-11-3
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Molecular Weight 468.43
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Formula C20H9D4F4N415NO2S
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SMILES
O=C([15NH2])C1=CC=C(N(C(N(C2=CC(C(F)(F)F)=C(C#N)N=C2)C3=O)=S)C43C([2H])([2H])CC4([2H])[2H])C=C1F
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
[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. [Content Brief]
[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 [Content Brief]
[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. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)