Androgen receptor antagonist 1

1338812-36-4

416.90

10 mM in DMSO

Others; PROTAC

Androgen receptor antagonist 1 is an orally available full androgen receptor (AR) antagonist with an IC₅₀ of 59 nM^[1]. Androgen receptor antagonist 1 (Compound 6) can be used in the synthesis of PROTAC AR degraders, which results 24% and 47 % AR protein degradation in LNCaP cells at 1 uM and 10 uM, respectively^[2]. IC50 & Target: IC50: 59 nM (androgen receptor)^[1] In Vitro: Androgen receptor antagonist 1 (Compound 26; 1 nM-100 uM) shows significant cell growth inhibition effects for LNCaP and LNAR cells but not DU145 cells^[1]. In Vivo: Androgen receptor antagonist 1 (Compound 26; 100 mg/kg once a day for 5 weeks) demonstrates excellent in vivo tumor growth inhibition upon oral administration in a castration-resistant prostate cancer (CRPC) animal model^[1].