N-desmethyl Enzalutamide|cas 1242137-16-1|DC Chemicals

N-desmethyl Enzalutamide|cas 1242137-16-1|DC Chemicals

N-desmethyl Enzalutamide(N-desmethyl MDV3100) is a major metabolite of Enzalutamide, Enzalutamide(MDV3100) is an androgen-receptor (AR) antagonist with IC50 of 36 nM.

IC50 value:

Target: androgen-receptor

Enzalutamide has greater affinity to AR than Bicalutamide does in a competition assay with 16β-[18F]fluoro-5α-DHT (18-FDHT) in castration-resistant LNCaP/AR cells (AR-overexpressing).

Product Name: N-desmethyl Enzalutamide|Cat No: DC9347|Cas: 1242137-16-1|Molecule Formular: C20H14F4N4O2S|Molecule Weight: 450.4094|Other names: N-desmethyl Enzalutamide

N-desmethyl Enzalutamide(N-desmethyl MDV3100) is a major metabolite of Enzalutamide, Enzalutamide(MDV3100) is an androgen-receptor (AR) antagonist with IC50 of 36 nM.
Enzalutamide has greater affinity to AR than Bicalutamide does in a competition assay with 16β-[18F]fluoro-5α-DHT (18-FDHT) in castration-resistant LNCaP/AR cells (AR-overexpressing). While Enzalutamide shows no agonism in LNCaP/AR prostate cells. Enzalutamide antagonizes induction of prostate-specific antigen (PSA) and transmembrane serine protease 2 (TMPRSS2), combination with the synthetic androgen R1881 in parental LNCaP cells. Enzalutamide could inhibit the transcriptional activity of a mutant AR protein (W741C, mutation of Trp741 to Cys). Enzalutamide also prevents nuclear translocation and co-activator recruitment of the ligand-receptor complex. Enzalutamide induces great tumor regression in castrate male mice bearing LNCaP/AR xenografts at a dose of 10 mg/kg.

For research only, not for human use!