MI-538

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Chemical Structure| 1857417-10-7 同义名 : -
CAS号 : 1857417-10-7
货号 : A461632
分子式 : C27H25F3N8OS
纯度 : 99%+
分子量 : 566.6
MDL号 : MFCD30532690
存储条件：

Pure form Keep in dark place, sealed in dry, store in freezer, under -20°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 : -
动物实验配方：
生物活性
描述 MI-538 stands out by inhibiting the growth of MLL leukemia cells, achieving a GI50 of 83 nM, and demonstrates specificity by not affecting the growth of HL-60 and HM-2 control cell lines, which lack MLL translocations, up to concentrations of 6 μM. This selectivity underscores its efficacy against cells transformed by MLL fusion proteins. MI-538's strong cellular activity is attributed to its low nanomolar affinity (Kd=6.5 nM) for menin, potentially enhanced by improved binding affinity and cellular uptake. Treatment with MI-538 significantly diminishes Hoxa9 and Meis1 gene expressions in MLL-AF9 cells, with about 100 nM reducing Hoxa9 expression by roughly 50% and even more substantially affecting Meis1 expression[1].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.76mL

0.35mL

0.18mL

8.82mL

1.76mL

0.88mL

17.65mL

3.53mL

1.76mL
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.