1242137-16-1

1242137-16-1 structure

Name: N-desmethyl Enzalutamide
Chemical Name: N-Desmethylenzalutamide
CAS Number: 1242137-16-1
Molecular Formula: C₂₀H₁₄F₄N₄O₂S
Molecular Weight: 450.40900
Catalog: Research Areas Cancer
Create Date: 2018-12-26 17:29:02
Modify Date: 2024-01-02 14:42:35
N-desmethyl Enzalutamide is the active metabolite of Enzalutamide. Enzalutamide is an androgen-receptor (AR) antagonist with IC50 of 36 nM in LNCaP cells.

Name	N-Desmethylenzalutamide
Synonyms	N-desmethyl Enzalutamide Enzalutamide Impurity 2

Description	N-desmethyl Enzalutamide is the active metabolite of Enzalutamide. Enzalutamide is an androgen-receptor (AR) antagonist with IC50 of 36 nM in LNCaP cells.
Related Catalog	Signaling Pathways >> Others >> Androgen Receptor Research Areas >> Cancer
Target	Androgen-receptor[1]
In Vivo	N-desmethyl Enzalutamide is an active metabolite that is thought to contribute to the clinical effects of Enzalutamide because it demonstrates primary and secondary pharmacodynamics of similar potency to Enzalutamide and circulates at approximately the same plasma concentrations as Enzalutamide. The carboxylic acid metabolite is pharmacologically inactive and circulates at approximately 25 % lower plasma concentrations than Enzalutamide[1].
References	[1]. Gibbons JA, et al. Pharmacokinetic Drug Interaction Studies with Enzalutamide. Clin Pharmacokinet. 2015 Oct;54(10):1057-69.