Apalutamide-d3

Modify Date: 2024-04-06 10:34:30

Apalutamide-d3 Structure
Apalutamide-d3 structure
Common Name Apalutamide-d3
CAS Number 1638885-61-6 Molecular Weight 480.45
Density N/A Boiling Point N/A
Molecular Formula C21H12D3F4N5O2S Melting Point N/A
MSDS N/A Flash Point N/A

 Use of Apalutamide-d3


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].

 Names

Name Apalutamide-d3

 Apalutamide-d3 Biological Activity

Description 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].
Related Catalog
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[1].
References

[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  

 Chemical & Physical Properties

Molecular Formula C21H12D3F4N5O2S
Molecular Weight 480.45