Description
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.
Uses
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].
in vivo
XY101 exhibits significant antitumor activities during the treatment period with tumor growth inhibition and is well tolerated without obvious body weight loss[1].
References
[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. DOI:
10.1021/acs.jmedchem.9b00327
![Benzeneacetamide, 4-(ethylsulfonyl)-N-[2'-fluoro-4'-[2,2,2-trifluoro-1-hydroxy-1-(trifluoromethyl)ethyl][1,1'-biphenyl]-4-yl]- Structure](https://www.chemicalbook.com/CAS/20200401/GIF/2349368-16-5.gif)
