| Bioactivity | Apalutamide-d3 is the deuterium labeled Apalutamide[1]. Apalutamide (ARN-509) is a potent and competitive androgen receptor (AR) antagonist, binding AR with an IC50 of 16 nM[2]. |
| Invitro | 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[1]. |
| Name | Apalutamide-d3 |
| CAS | 1638885-61-6 |
| Formula | C21H12D3F4N5O2S |
| Molar Mass | 480.45 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019 Feb;53(2):211-216. [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 |
Apalutamide-d3
CAS: 1638885-61-6 F: C21H12D3F4N5O2S W: 480.45
Apalutamide-d3 is the deuterium labeled Apalutamide. Apalutamide (ARN-509) is a potent and competitive androgen receptor
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