M-1211

CAS: 2377337-93-2 货号: M649123 分子式: C42H57FN6O6S 分子量: 793.00
有货
级别和纯度: ≥99%
储存条件
避光,-20°C储存,干燥
运输条件
超低温运输
★
规格
库存
价格
数量
1mg
M649123-1mg
期货 Stock Image
¥11,800.90
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概述


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

In Vitro

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

In Vivo

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% . 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 . M-1121 (5 mg/kg; p.o.) has a low clearance and a moderate volume of distribution . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: SCID mice 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 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 Dosage: 5 mg/kg (Pharmacokinetic Analysis) Administration: P.o. Result: Had a low clearance and a moderate volume of distribution.

Form:Solid

IC50& Target:menin-MLL interaction

规格

规格或纯度
≥99%
英文名称
M-1211
生化机理
M-1121 是一种具有共价和口服活性的 Menin-MLL 相互作用抑制剂,能够实现肿瘤的完全和持续消退。
储存条件
避光,-20°C储存,干燥
运输条件
超低温运输
作用类型
抑制剂
纯度
≥99%
名称和识别符
分子类型
小分子
分子量
793.00

高级数据

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常见问题

本产品的纯度是多少?
本产品的化学纯度(含量)为 ≥99%。批次的具体数值以分析证书(COA)为准。
本产品应如何储存?
请于?20 °C、避光、干燥条件下保存。请与干燥剂一同密封保存,本品对湿气敏感。
本产品如何运输?
本产品采用保温箱配冰袋运输。收货后请立即拆包,并按上述储存条件保存。
本产品的 CAS 号、分子式和分子量是多少?
本产品的 CAS 号为 2377337-93-2,分子式为 C42H57FN6O6S,分子量为 793.00 g/mol。
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