Apalutamide-d7

Apalutamide-d7 is deuterated labeled Apalutamide (HY-16060) . Apalutamide (ARN-509) is a potent and competitive androgen receptor (AR) antagonist, binding AR with an IC50 of 16 nM[1].

Product Specifications

Product Name Alternative

ARN-509-d7

UNSPSC

12352005

Target

Androgen Receptor; Isotope-Labeled Compounds

Type

Isotope-Labeled Compounds

Related Pathways

Others; Vitamin D Related/Nuclear Receptor

Applications

Cancer-programmed cell death

Field of Research

Cancer

Solubility

10 mM in DMSO

Smiles

O=C(NC([2H])([2H])[2H])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

Molecular Formula

C21H8D7F4N5O2S

Molecular Weight

484.48

References & Citations

[1]Clegg NJ, et al. ARN-509: a novel antiandrogen for prostate cancer treatment. Cancer Res. 2012 Mar 15;72 (6) :1494-503.|[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]Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019 Feb;53 (2) :211-216.