Name: FK 866 hydrochloride
Price: 228.00 USD

- Overview
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    Background
    
    FK 866 hydrochloride is an inhibitor of nicotinamide phosphoribosyltransferase (NMPRTase) with IC50 values ranging between 0.09nM and 27.2nM [1]. NAD plays a vital role in numerous biochemical and biologic processes. Targeting NAD synthesis is thought to be a selective manner to kill cancer cells since cancer cells have a higher rate of NAD turnover compared with normal cells. In the vitro MTT assay using a panel of 41 human hematologic cancer cell lines, most cancer cells are sensitive to low concentrations of FK866. Among these cancer cells, AML cells are most sensitive. FK866 is shown selective to human hematologic malignant cells and the normal human HPCs are resistant to FK866 treatment. It is found that FK866 induces cell death in a caspase-independent pathway but in a dose-dependent manner to induce mitochondrial membrane depolarization. Additionally, FK866 induces cell autophagy dependenting on de novo protein synthesis. FK866 also reduces ATP levels in ML-2 cells due to the inhibition of NAD synthesis. The antitumor efficacy of FK866 is also shown in the in vivo models. FK866 significantly prevents tumor growth both in mice xenografted subcutaneously with AML-M4 and Namalwa cells. Furthermore, FK866 clears tumor cells to below detectable levels and results in 80% survival for a long-term [1].
- Properties
  - Alternative Name
    
    (E)-N-(4-(1-benzoylpiperidin-4-yl)butyl)-3-(pyridin-3-yl)acrylamide hydrochloride
    
    CAS Number
    
    658084-64-1 (free base)
    
    Molecular Formula
    
    C24H30ClN3O2
    
    Molecular Weight
    
    427.97
    
    Appearance
    
    A solid
    
    Purity
    
    99.87%
    
    Solubility
    
    ≥18.95 mg/mL in DMSO; ≥21 mg/mL in EtOH; ≥9.8 mg/mL in H2O
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only