GSK126 在雌性米色 SCID 小鼠中以每 20 g 体重 0.2 mL 的剂量体积腹腔注射给药。GSK126有效抑制EZH2突变DLBCL细胞系的增殖,并显着抑制EZH2突变DLBCL异种移植物在小鼠体内的生长[1]。
参考文献
[1]. McCabe MT, et al. EZH2 inhibition as a therapeutic strategy for lymphoma with EZH2-activating mutations. Nature. 2012 Dec 6;492(7427):108-12.
[2]. Sato T, et al. PRC2 overexpression and PRC2-target gene repression relating to poorer prognosis in small cell lung cancer. Sci Rep. 2013 May 29;3:1911.
[1]. McCabe MT, et al. EZH2 inhibition as a therapeutic strategy for lymphoma with EZH2-activating mutations. Nature. 2012 Dec 6;492(7427):108-12.
[2]. Sato T, et al. PRC2 overexpression and PRC2-target gene repression relating to poorer prognosis in small cell lung cancer. Sci Rep. 2013 May 29;3:1911.