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XY101
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
XY101图片
CAS NO:2349368-16-5

XY101 是一种有效选择性的、代谢稳定的口服 RORγ 反向激动剂,IC50 为 30 nM,Kd 为 380 nM。
Cas No.2349368-16-5
Canonical SMILESO=S(C1=CC=C(CC(NC2=CC=C(C3=C(F)C=C(C(O)(C(F)(F)F)C(F)(F)F)C=C3)C=C2)=O)C=C1)(CC)=O
分子式C25H20F7NO4S
分子量563.48
溶解度DMSO: 250 mg/mL (443.67 mM)
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

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.

 
 
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