XY-018

XY-018 is an inverse agonist of retinoic acid receptor-related orphan receptor gamma (RORgamma). It induces RORgamma transcriptional activity in a reporter assay using LNCaP cells (IC50 = 0. µM). XY-018 selectively induces RORgamma transcriptional activity over RORalpha transcriptional activity in HEK293T cells (IC50 = 7. µM). It reduces the proliferation of androgen receptor-positive LNCaP, 22Rv1, and C4-2B and androgen receptor-negative DU145 and PC3 prostate cancer cells (IC50s = 5. 9, 9. 28. and 11. µM, respectively). XY-018 (40 mg/kg per day) decreases tumor volume and induces apoptosis in a patient-derived xenograft (PDX) mouse model of castration-resistant prostate cancer.. Solulibility: Acetonitrile: Slightly Soluble: 0.1-1 mg/ml: .