M-808 T39937

Product Introduction
Bioactivity


英文名: M-808

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.

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].

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

关键字: M-808 | M 808 | M808

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途