EPZ004777CAS号： 1338466-77-5分子式： C28H41N7O4分子量： 539.67描述纯度储存/保存方法别名外观可溶性/溶解性靶点In vitro(体外研究)In vivo(体内研究)
| 产品描述 | |
| 描述 |
EPZ004777 is a potent, selective inhibitor of DOT1L. EPZ004777 selectively inhibits cellular H3K79 methylation and inhibits expression of key MLL fusion target genes. |
| 纯度 |
>98%
|
| 储存/保存方法 |
Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.
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| 基本信息 | |
| 别名 |
EPZ 004777；EPZ-004777
|
| 外观 |
powder
|
| 可溶性/溶解性 |
DMSO : 54 mg/mL (100 mM)
Ethanol : 54 mg/mL (100 mM) |
| 生物活性 | |
| 靶点 |
DOT1L
|
| In vitro(体外研究) |
EPZ004777 selectively inhibits cellular H3K79 methylation and inhibits expression of key MLL fusion target genes. Following DOT1L inhibition, EPZ004777 selectively inhibits proliferation of MLL-Rearranged cell lines and MLL-AF9-transformed murine hematopoietic cells. In addition, EPZ004777 also induces differentiation and apoptosis in MLL-rearranged cells. EPZ004777 selectively inhibits proliferation of MLL–AF10 and CALM–AF10-transformed murine bone marrow cells. DOT1L inhibition by EPZ004777 results in significantly decreased proliferation, decreased expression of MLL-AF6 target genes, and cell cycle arrest of MLL-AF6-transformed cells.
|
| In vivo(体内研究) |
EPZ004777 produces potent antitumor efficacy, and significantly increases median survival in a mouse xenograft model of MLL leukemia.
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分子结构图
