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M-808 is a potent and efficacious covalent inhibitor, targeting the interaction between Menin and MLL. It demonstrates a high binding affinity with an IC50 value of 2.6 nM.

M-808 is a potent and efficacious covalent inhibitor, targeting the interaction between Menin and MLL. It demonstrates a high binding affinity with an IC50 value of 2.6 nM.
| 规格 | 价格 | 库存 | 数量 |
|---|---|---|---|
| 25 mg | ¥ 69,000 | 6-8周 |
M-808 相关产品
| 产品描述 | M-808 is a potent and efficacious covalent inhibitor, targeting the interaction between Menin and MLL. It demonstrates a high binding affinity with an IC50 value of 2.6 nM. |
| 靶点活性 | MV-4-11 cells:1 nM (IC50), Menin-MLL (MOLM-13 cells):4 nM (IC50), Menin-MLL (MV4):1 nM (IC50) |
| 体外活性 | M808 exhibits IC 50 values of 1 nM, 4 nM and 2.8 nM in MV4;11 cells, MOLM-13 cells and HL60 cells, respectively[1]. M808 forms a covalent bond between its acrylamide and the sulfur atom of Cys329 in menin[1]. |
| 体内活性 | M-808 (16) is well tolerated in severe combined immunodeficiency (SCID) mice with intravenous administration of 10 mg/kg (or 25 mg/kg) every other day dosing (three times a week) for one week. M-808 (25 mg/kg) achieves a maximum tumor growth inhibition (TGI) of 97% during treatment (day 35) and reduces the average tumor volume from 92 mm 3 at the beginning of the treatment to 59 mm 3 at day 35, with no significant toxicity[1]. |
| 分子量 | 819.09 |
| 分子式 | C45H63FN6O5S |
| CAS No. | 2377335-74-3 |
| 存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
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