Name: MI-136
Price: 461.00 USD

- Overview
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    Background
    
    IC50: 31 nMMI-136 is a menin-MLL interaction inhibitor.Chromosomal translocations regulating mixed lineage leukemia gene (MLL) can result in the acute leukemias resistant to therapy. The leukemogenic activity of MLL fusion protein is reported to be dependent on its interactions with menin, providing the basis for therapeutic intervention. In vitro: MI-136 was found to be able to strongly bind to menin with Kd of 24 nM, potently inhibit menin interaction with MLL, and block proliferation of MLL leukemia cells at submicromolar concentrations (GI50 = 0.55 μM in the MLL-AF9 cells), indicating that MI-136 represented a valuable pharmacophore for menin-MLL inhibitors. In addition, MI-136 did not show substantial off-target activity when profiled on a panel of kinases and GPCRs [1]. In vivo: Animal study showed that treatment of VCaP tumor–bearing mice with MI-136 at 40 mg/kg resulted in a modest but significant reduction in tumor volume when compared to vehicle treatment with no effect on body weight of mouse. These data demonstrated that the pharmacologic inhibition of the menin-MLL interaction was an effective in vivo treatment for MLL leukemias and provided advanced molecular scaffold for clinical lead identification [2]. Clinical trial: Up to now, MI-136 is still in the preclinical development stage.
    
    1. D. Borkin, J. Pollock, K. Kempinska,et al.Property focused structure-based optimization of small molecule inhibitors of the protein-protein interaction between menin and mixed lineage leukemia (MLL). Journal of Medicinal Chemistry 59(3),892-913(2016).
    2. R. Malik, A. P. Khan, I. A. Asangani,et al. Targeting the MLL complex in castration-resistant prostate cancer.Nat. Med.21(4),344-352(2015).
- Properties
  - Alternative Name
    
    5-((4-((6-(2,2,2-trifluoroethyl)thieno[2,3-d]pyrimidin-4-yl)amino)piperidin-1-yl)methyl)-1H-indole-2-carbonitrile
    
    CAS Number
    
    1628316-74-4
    
    Molecular Formula
    
    C23H21F3N6S
    
    Molecular Weight
    
    470.51
    
    Appearance
    
    A crystalline solid
    
    Purity
    
    98.00%
    
    Solubility
    
    Soluble in DMSO
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only

MI-136

MI-136

Background

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