产品号 #100-1655_C
组蛋白修饰剂；抑制端粒沉默中断物1-like （DOT1L）
EPZ004777（甲酸盐）可诱导多种癌细胞的抗肿瘤效应。EPZ004777（甲酸盐）是一种强效的端粒沉默破坏因子1 (DOT1) 样组蛋白赖氨酸甲基转移酶 (DOT1L；IC50 = 400 pM) 抑制剂。通过抑制 DOT1L，EPZ004777（甲酸盐）可阻止 DOT1L 介导的组蛋白 3 第 79 位赖氨酸甲基化 (H3K79; Daigle et al. Cancer Cell, 2011)。众所周知，甲基化会影响端粒沉默、转录调控、DNA 损伤修复和细胞周期进程 (Nguyen & Zhang. Genes Dev, 2011)。 DOTL1 介导的 H3K79 甲基化失调与混合谱系白血病 (MLL) 的发展以及其他癌症的病理生理有关 (McLean et al. Leukemia, 2014)。
EPZ004777（甲酸盐）已用于：
癌症研究
·降低人类前列腺癌细胞系和患者来源的异种移植模型中的细胞活力和集落形成（Vatapalli et al. Nat Commun, 2020)。
·在小鼠卵巢癌和人卵巢癌细胞系异种移植模型中抑制细胞生长并上调促凋亡基因（Vatapalli et al. Nat Commun, 2020)。
·在小鼠异种移植模型中降低小鼠胰腺癌和结肠癌细胞活力和集落形成，并降低肿瘤生长（Zhou et al. Mol Oncol, 2019)。
·在小鼠异种移植模型中诱导人类急性髓系白血病细胞凋亡、细胞周期阻滞和终末分化，并抑制白血病肿瘤生长（Zhou et al. Mol Oncol, 2019)。
EPZ004777（甲酸盐）已用于：
癌症研究
·降低人类前列腺癌细胞系和患者来源的异种移植模型中的细胞活力和集落形成（Vatapalli et al. Nat Commun, 2020)。
·在小鼠卵巢癌和人卵巢癌细胞系异种移植模型中抑制细胞生长并上调促凋亡基因（Vatapalli et al. Nat Commun, 2020)。
·在小鼠异种移植模型中降低小鼠胰腺癌和结肠癌细胞活力和集落形成，并降低肿瘤生长（Zhou et al. Mol Oncol, 2019)。
·在小鼠异种移植模型中诱导人类急性髓系白血病细胞凋亡、细胞周期阻滞和终末分化，并抑制白血病肿瘤生长（Zhou et al. Mol Oncol, 2019)。
Protocols and Documentation
Find supporting information and directions for use in the Product Information Sheet or explore additional protocols below.
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| Molecular Weight | 585.7 g/mol |
|---|---|
| Alternative Names | Not applicable |
| Cas Number | Not applicable |
| Chemical Formula | C28H41N7O4 • CH2O2 |
| Purity | ≥ 98% |
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