MI-538

    
98%

MI-538

源叶(MedMol)
S84091 一键复制产品信息
1857417-10-7
C27H25F3N8OS
566.6006
货号 规格 价格 上海 北京 武汉 南京 购买数量
S84091-1mg 98% ¥1100.00 货期:2-3天 - - -
S84091-5mg 98% ¥2400.00 货期:2-3天 - - -
S84091-10mg 98% ¥4200.00 货期:2-3天 - - -
产品介绍 参考文献 质检证书(COA) 摩尔浓度计算器 相关产品

产品介绍

MI-538 is an inhibitor of the interaction between menin and MLL fusion proteins with an IC50 of 21 nM

产品描述: MI-538 is an inhibitor of the interaction between menin and MLL fusion proteins with an IC50 of 21 nM
靶点: IC50 : 21 nM (menin and MLL interaction); Kd: 6.5 nM (menin);EpigeneticReaderDomain; HistoneMethyltransferase
体外研究: MI-538 inhibits the proliferation of MLL leukemia cells with a GI50 of 83 nM. MI-538 shows no effect (up to 6 μM) on growth of the control cell lines HL-60 and HM-2, which do not harbor MLL translocations, demonstrating good selectivity toward MLL fusion protein transformed cells. MI-538 binds to menin with low nanomolar affinity (Kd=6.5 nM). Its potent cellular activity originates from the improved binding affinity to menin and possibly increased cell membrane permeability. Treatment with MI-538 results in strong down regulation of expression of Hoxa9 and Meis1 genes. About 100 nM 27 was sufficient to reduce by ~50% Hoxa9 expression in MLL-AF9 cells, and even more pronounced effect was seen on Meis1 expression
体内研究: Treatment with MI-538 results in a pronounced, about 80%, reduction in the MV4;11 tumor volume, without causing substantial signs of toxicity reflected by less than 10% reduction of the body weight. MI-538 demonstrates markedly improved exposure (area under the curve, AUC, values), Cmax (maximum compound concentration) in the blood plasma, and the lowest value of clearance. The half-life of MI-538 is about 1.6 h. MI-538 has also high oral bioavailability (~50%)
参考文献: 1. Borkin D, et al. Property Focused Structure-Based Optimization of Small Molecule Inhibitors of the Protein-Protein Interaction between Menin and Mixed Lineage Leukemia (MLL). J Med Chem. 2016 Feb 11;59(3):892-913.
溶解性: soluble  in  DMSO
保存条件: -20℃
配置溶液浓度参考:
1mg 5mg 10mg
1 mM 1.765 ml 8.825 ml 17.649 ml
5 mM 0.353 ml 1.765 ml 3.53 ml
10 mM 0.176 ml 0.882 ml 1.765 ml
50 mM 0.035 ml 0.176 ml 0.353 ml
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参考文献

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