Benzeneacetamide, 4-(ethylsulfonyl)-N-[2'-fluoro-4'-[2,2,2-trifluoro-1-hydroxy-1-(trifluoromethyl)ethyl][1,1'-biphenyl]-4-yl]-

XY101 is a Potent, Selective, and Orally Bioavailable RORγ Inverse Agonist for Treatment of Castration-Resistant Prostate Cancer with IC50 = 30nM. XY101 potently inhibited cell growth, colony formation, and the expression of AR, AR-V7, and PSA. XY101 also exhibited good metabolic stability and a pharmacokinetic profile with oral bioavailability of 59% and a half-life of 7.3 h. Notably, XY101 demonstrated promising therapeutic effects with significant tumor growth inhibition in a prostate cancer xenograft model inmice.