M-1211 T39938

Product Introduction
Bioactivity


英文名: M-1211

描述: M 1121 is a covalent and orally active inhibitor of the menin-MLL interaction capable of achieving complete and persistent tumor regression.

体外活性: 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]. RT-PCR[1]Cell Line: MV4;11 cells Concentration: 0~100 nM Incubation Time: 24 hours Result: Drived dose-dependent down-regulation of HOXA9 and MEIS1 gene expression in the MLL-rearranged MV4;11 leukemia cell line.

体内活性: M-1121 (100 mg/kg; p.o.; 26 days) reduces the average tumor volume from 157 mm 3 at the beginning of the treatment to 106 mm 3 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]. Animal Model: SCID mice[1]Dosage: 100 mg/kg Administration: P.o. Result: Reduced the average tumor volume from 157 mm 3 at the beginning of the treatment to 106 mm 3 on day 26 of the treatment, a reduction of tumor volume of 32%. Animal Model: SCID mice[1]Dosage: 300 mg/kg Administration: P.o. Result: Led to complete tumor regression in 10 out of 10 mice with no tumor regrowth detected up to a month after last treatment. Animal Model: Female C57BL/6 mice[1]Dosage: 5 mg/kg (Pharmacokinetic Analysis) Administration: P.o. Result: Had a low clearance and a moderate volume of distribution.

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

关键字: M 1211 | M1211 | M-1211

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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