化合物MI-463 TQ0058

Product Introduction
Bioactivity


英文名: MI-463

描述: MI-463 是一种有口服活性的menin-mLL 相互作用的高效小分子抑制剂，IC50为15.3 nM。

细胞实验: Leukemia cells are treated with MI-463 or 0.25% DMSO and cultured at 37 °C for 7 days. Media is changed on day 4, viable cell numbers are restored to the original concentration and MI-463 is re-supplied. MTT cell proliferation assay kit is then employed, and plates are read for absorbance at 570 nm using a microplate reader.

动物实验: For efficacy studies in MV4;11 subcutaneous xenograft mice model, 5×10^6 cells are injected into the 4-6 week old female BALB/c nude mice. Treatment is started when the tumor size reached ~100 mm^3. Vehicle (25% DMSO, 25% PEG400, 50% PBS) or MI-463 are administrated once daily at designated doses using i.p. injections.

体外活性: 将含有mLL-AF9癌基因的鼠骨髓细胞（BMC）用MI-463处理可显著抑制其增长（GI50：0.23 μM）。MI-463能有效诱导MLL白血病细胞分化。使用低于微摩尔浓度的MI-463还能显著降低Hoxa9和Meis1的表达。

体内活性: MI-463在MLL白血病的小鼠模型中显示出显著的生存益处。该化合物具有非常有利的类药性质，包括在小鼠中的代谢稳定性和PK概况。单次静脉或口服给药后，MI-463在外周血中达到高浓度，同时展示高口服生物利用度（45%）。通过每天一次的腹腔内（i.p.）给药，MI-463强烈抑制肿瘤生长。在MI-463处理后，目标基因mLL融合蛋白的表达，包括HOXA9和MEIS1，显著降低。

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

溶解度: DMSO : 120 mg/mL (247.66 mM)


关键字: Epigenetic Reader Domain | Inhibitor | MI 463 | MI-463 | inhibit | MI463

相关产品: OF-1 | BRM/BRG1 ATP Inhibitor-2 | GSK737 | CPI-637 | FKBP12 PROTAC dTAG-7 | GSK778 | BRD4 Inhibitor-10 | GSK778 hydrochloride | GNE-375 | BY27

相关库: Anti-Aging Compound Library | Bioactive Compounds Library Max | Inhibitor Library | Epigenetics Compound Library | PPI Inhibitor Library | Stem Cell Differentiation Compound Library | Reprogramming Compound Library | Methylation Compound Library | Histone Modification Compound Library | Chromatin Modification Compound Library

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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