M-1211 

M‑1121 is a covalent and orally active inhibitor of the menin-MLL interaction capable of achieving complete and persistent tumor regression^[1].

menin-MLL interaction^[1]

M-1121 (0~100 nM; 24 hours; MV4;11 cells) drives dose-dependent down-regulation of HOXA9 and MEIS1 gene expression in the MLL-rearranged MV4;11 leukemia cell line^[1].
M-1121 establishes covalent interactions with Cysteine 329 located in the MLL binding pocket of menin and potently inhibits growth of acute leukemia cell lines carrying MLL translocations with no activity in cell lines with wild-type MLL^[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

M-1121 (100 mg/kg; p.o.; 26 days) reduces the average tumor volume from 157 mm³ at the beginning of the treatment to 106 mm³ on day 26 of the treatment, a reduction of tumor volume of 32%^[1].
M-1121 (300 mg/kg; p.o.) leads to complete tumor regression in 10 out of 10 mice with no tumor regrowth detected up to a month after last treatment^[1].
M-1121 (5 mg/kg; p.o.) has a low clearance and a moderate volume of distribution^[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

793.00

C₄₂H₅₇FN₆O₆S

2377337-93-2

固体

White to yellow

Room temperature in continental US; may vary elsewhere.

-20°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

• [1]. Zhang M, et al. Discovery of M-1121 as an Orally Active Covalent Inhibitor of Menin-MLL Interaction Capable of Achieving Complete and Long-Lasting Tumor Regression. J Med Chem. 2021;64(14):10333-10349.  [Content Brief]