| Description | XY101 is a selective, metabolically stable and orally available agonist of RORγ inverse(IC50 of 30 nM and a Kd of 380 nM). |
| In vitro | XY101有效抑制细胞生长、集落形成以及雄激素受体(AR)、AR-V7和前列腺特异性抗原(PSA)的表达[1]。 |
| In vivo | XY101在治疗期间展现了显著的抗肿瘤活性,能够抑制肿瘤生长,并具有良好的耐受性,未出现明显的体重减轻[1]。 |
| Target activity | RORγ:(kd)380 nM , RORγ:30 nM |
| molecular weight | 563.48 |
| Molecular formula | C25H20F7NO4S |
| CAS | 2349368-16-5 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 225 mg/mL (399.3 mM), Sonication is recommended. |
| References | 1. ng 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. |