| 产品描述: | Menin-MLL inhibitor-22 (compound C20) is an orally active inhibitor of the interaction between menin and mixed lineage leukemia (MLL) (IC50=7 nM). Menin-MLL inhibitor-22 binds menin protein and inhibits cancer cell growth (MV4 cells, IC50=0.3 μM). Menin is a putative tumor suppressor associated with multiple endocrine neoplasia type 1 (MEN-1 syndrome). |
| 体外研究: |
Menin-MLL inhibitor-22 (1 μM; 60 min) possesses good stability and low clearance rate in liver microsomes. Menin-MLL inhibitor-22 (1 and 10 μM; 24 h) inhibits MLL-r Leukemia cells MV4;11 growth and (0.1-10 μM; 24 h) decreases the expression of the HOXA9 and MEIS1 induced by menin-MLL interaction. Menin-MLL inhibitor-22 (1, and 10 μM; 7 d) increases the amount of CD11b, a differentiation marker of myeloid cells, indicating a reverse the differentiation arrest of MLL-r leukemia cells. Menin-MLL inhibitor-22 (1, and 10 μM; 24 h) induces cell apoptosis and G0/G1 cell cycle arrest. |
| 体内研究: |
Menin-MLL inhibitor-22 (6 mg/kg and 30 mg/kg; p.o.; every second day for 16 days) shows potent antitumor activity in the MV4;11 subcutaneous xenograft models of MLL-rearranged leukemia.
Pharmacokinetic Properties in SD Rats |
| 参考文献: |
1. Lei H, et al. Discovery of Novel, Potent, and Selective Small-Molecule Menin-Mixed Lineage Leukemia Interaction Inhibitors through Attempting Introduction of Hydrophilic Groups. J Med Chem. 2022 Oct 13;65(19):13413-13435.
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| 保存条件: |
-20°C |
| 配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
| 1 mM |
1.768 ml |
8.838 ml |
17.676 ml |
| 5 mM |
0.354 ml |
1.768 ml |
3.535 ml |
| 10 mM |
0.177 ml |
0.884 ml |
1.768 ml |
| 50 mM |
0.035 ml |
0.177 ml |
0.354 ml |
|
| 注意: |
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