EPZ6438

一种口服生物可利用的EZH2选择性抑制剂（Ki=2.5nM）；阻断野生型和突变型淋巴瘤细胞中的H3K27三甲基化（IC50范围为2-90nM）；特异性地诱导SMARCB1删除的恶性横纹肌样肿瘤细胞凋亡和分化，并促进异种移植小鼠中的肿瘤消退。An orally bioavailable, selective inhibitor of EZH2 (Ki = 2.5 nM); blocks H3K27 trimethylation in both wild-type and mutant lymphoma cells (IC50s range from 2-90 nM); induces apoptosis and differentiation specifically in SMARCB1-deleted malignant rhabdoid tumor cells and promotes their regression in xenograft-bearing mice.