Powder: -20°C for 3 years | In solvent: -80°C for 1 year
M 1121 is a covalent and orally active inhibitor of the menin-MLL interaction capable of achieving complete and persistent tumor regression.
产品描述 | 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. |
分子量 | 793.01 |
分子式 | C42H57FN6O6S |
CAS No. | 2377337-93-2 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
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