XY101 is a potent, selective, metabolically stable and orally available RORγ inverse agonist with an IC50 of 30 nM and a Kd of 380 nM.IC50 & Target: IC50: 30 nM (RORγ)
Kd: 380 nM (RORγ)In Vitro: XY101 potently inhibits cell growth, colony formation, and the expression of androgen receptor (AR), AR-V7 and prostate-specific antigen (PSA).In Vivo: XY101 exhibits significant antitumor activities during the treatment period with tumor growth inhibition and is well tolerated without obvious body weight loss.