Androgen receptor antagonist 1 is an orally available full androgen receptor antagonist (IC50: 59 nM). It can be used in the synthesis of PROTAC AR degraders, which results in 24% and 47 % AR protein degradation in LNCaP cells at 1 μM and 10 μM, respectively.

Androgen receptor antagonist 1 (Compound 26; 1 nM-100 μM) shows significant cell growth inhibition effects for LNAR and LNCaP cells but not DU145 cells [1].

Androgen receptor antagonist 1 (100 mg/kg once a day for 5 weeks) shows excellent in vivo tumor growth inhibition upon oral administration in castration-resistant prostate cancer (CRPC) animal model [1].

1338812-36-4

C21H25ClN4O3

416.9

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years