生物活性 | |||
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描述 | VTP50469 is a potent, highly selective and orally active inhibitor of Menin-MLL interaction with a Ki value of 104 pM. VTP50469 exhibits potent antileukaemic activity[1][2].At early time points, the MLL-r B-cell ALL (B-ALL) cell line, but not the MLL-r AML cell line, responds apoptotically to VTP50469 in a dose-dependent manner. The MLL-r AML cell line begins to dose-dependently differentiate after 4-6 days of exposure to VTP50469[1].VTP50469 displaces Menin from the protein complex and inhibits chromatin occupancy by MLL at specific genes. Loss of binding to MLL results in changes in gene expression, differentiation and apoptosis[1]. |
实验方案 | |||
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1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
1.59mL 0.32mL 0.16mL |
7.93mL 1.59mL 0.79mL |
15.85mL 3.17mL 1.59mL |