PF-06726304
规格
| Cas Number | 1616287-82-1 |
| 规格或纯度 | 10mM in DMSO |
| 包装 | 1ml |
产品信息
| 品牌 | 阿拉丁 |
| 浓度 | 10mM in DMSO |
| 简短描述 | EZH1/2 抑制剂 |
| 英文简短描述 | EZH1/2 Inhibitors |
| 过滤标签 | Compound libraries |
| 储存温度 | -80℃储存 |
| 运输条件 | 超低温冰袋运输 |
| 生化和生理学机理 | PF-06726304 是一种选择性 EZH2 抑制剂，对 WT EZH2 和 Y641N 的 Ki 值分别为 0.7 nM 和 3 nM；还能抑制 H3K27me3，IC50 值为 15 nM。 |
| 英文描述 |
Information PF-06726304 PF-06726304 is a selective EZH2 inhibitor with Ki values of 0.7 nM and 3 nM for WT EZH2 and Y641N respectively; also inhibits H3K27me3 with the IC50 value of 15 nM. Targets Ezh2 (wild-type) (cell-free); EZH2 Y641N (cell-free) 0.7 nM(Ki); 3 nM(Ki) In vitro PF-06726304 displays very potent EZH2 biochemical inhibition as well as good activity in the cell H3K27Me3 reduction and antiproliferation effect. In vivo PF-06726304 displays robust in vivo antitumor growth activity and dose-dependent de-repression of EZH2 target genes. PF-06726304 displays good efficacy in a diffuse large B-cell lymphoma Karpas-422 tumor model and exhibited on-target pharmacodynamic effects in vivo. Cell Research(from reference) Cell lines：Karpas-422 cell line Incubation Time：72 h |