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[1]. IC50: 30 nM (RORγ)[1]Kd: 380 nM (RORγ)[1]
XY101 potently inhibits cell growth, colony formation, and the expression of androgen receptor (AR), AR-V7 and prostate-specific antigen (PSA)[1].
XY101 exhibits significant antitumor activities during the treatment period with tumor growth inhibition and is well tolerated without obvious body weight loss[1].
[1]. Zhang Y, et al. Discovery and Characterization of XY101, a Potent, Selective, and Orally Bioavailable RORγ Inverse Agonist for Treatment of Castration-Resistant Prostate Cancer. J Med Chem. 2019 May 9;62(9):4716-4730.