Enzalutamide

Research use only, not for human use.

An androgen-receptor (AR) antagonist with IC50 of 36 nM.

An androgen-receptor (AR) antagonist with IC50 of 36 nM; reduces the efficiency of AR nuclear translocation, and impairs both DNA binding to androgen response elements and recruitment of coactivators; induces tumor regression in mouse models of castration-resistant human prostate cancer; orally available.Prostate cancer Approved(In Vitro):Enzalutamide (MDV3100) has greater affinity to AR than ICI 176334 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 inhibits 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.(In Vivo):Enzalutamide (MDV3100) induces great tumor regression in castrate male mice bearing LNCaP/AR xenografts at a dose of 10 mg/kg.Enzalutamide shows dose-independent pharmacokinetics at intravenous and oral doses of 0.5-5 mg/kg.

——

——

MDV3100 | MDV-3100 | MDV 3100

Endocrinology/Hormones

Androgen Receptor (AR)

AndrogenReceptor

Cancer

Prostate Cancer

915087-33-1

464.4359

C21H16F4N4O2S

>98% (HPLC)

10 mM in DMSO

O=C(NC)C1=CC=C(N(C(N2C3=CC=C(C#N)C(C(F)(F)F)=C3)=S)C(C)(C)C2=O)C=C1F

Benzamide, 4-[3-[4-cyano-3-(trifluoromethyl)phenyl]-5,5-dimethyl-4-oxo-2-thioxo-1-imidazolidinyl]-2-fluoro-N-methyl-

(-20℃)

With Ice Pack

≥ 2 years