RORγ antagonist (EC50 = 190 nM). Suppresses androgen receptor expression in prostate cancer cell lines. Also inhibits growth of tumors in androgen receptor-positive xenograft models.
Wang et al (2016) ROR-γ drives androgen receptor expression and represents a therapeutic target in castration-resistant prostate cancer. Nat.Med. 22 488 PMID:27019329 |Ndagi et al (2016) Re-emergence of an orphan therapeutic target for the treatment of resistant prostate cancer - a through conformational and binding analysis for RORγ protein. J.Biomol.Struct.Dyn. 36 1