Name: FK866 (APO866)
Price: 204.00 USD

- Overview
  - Please contact us at for specific academic pricing.
    
    Background
    
    FK866 is an inhibitor of nicotinamide phosphoribosyltransferase (NMPRTase) with IC50 values ranging between 0.09 nM and 27.2 nM [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 in 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].
    
    [1] Nahimana A, Attinger A, Aubry D, Greaney P, Ireson C, Thougaard AV, Tjørnelund J, Dawson KM, Dupuis M, Duchosal MA. The NAD biosynthesis inhibitor APO866 has potent antitumor activity against hematologic malignancies. Blood. 2009 Apr 2; 113 (14): 3276-86.
- Properties
  - Alternative Name
    
    (E)-N-[4-(1-benzoylpiperidin-4-yl)butyl]-3-pyridin-3-ylprop-2-enamide
    
    CAS Number
    
    658084-64-1
    
    Molecular Formula
    
    C24H29N3O2
    
    Molecular Weight
    
    391.51
    
    Appearance
    
    A solid
    
    Purity
    
    99.57%
    
    Solubility
    
    insoluble in H2O; ≥19.6 mg/mL in DMSO; ≥49.6 mg/mL in EtOH
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only
- Reference
  - 1. Qingrui Zhuan, Jun Li, et al. "Nampt affects mitochondrial function in aged oocytes by mediating the downstream effector FoxO3a." J Cell Physiol. 2022 Jan;237(1):647-659. PMID:34318928
    2. Juvita D Iljas, Zhe Wei, et al. "Sirt1 sustains female fertility by slowing age‐related decline in oocyte quality required for post‐fertilization embryo development." Aging Cell. 2020;00:e13204. PMID:32729989
    3. Zhe Wei, Jessica Greaney, et al. "Nampt-mediated spindle sizing secures a post-anaphase increase in spindle speed required for extreme asymmetry." Nature Communications volume 11, Article number: 3393 (2020);07 July 2020. PMID:32636388
    4. Huang Y, Peng Y, et al. "Nicotinamide Phosphoribosyl Transferase Controls NLRP3 Inflammasome Activity Through MAPK and NF-κB Signaling in Nucleus Pulposus Cells, as Suppressed by Melatonin." Inflammation. 2020;10.1007/s10753-019-01166-z. PMID:31900828
    5. Shi KL, Qian JY, et al. "Atorvastatin antagonizes the visfatin-induced expression of inflammatory mediators via the upregulation of NF-κB activation in HCAECs." Oncol Lett. 2016 Aug;12(2):1438-1444. PMID:27446449

FK866 (APO866)

FK866 (APO866)

Background

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