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    FK866 (APO866, Daporinad)
    FK866 (APO866, Daporinad)

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V0917
    CAS #: 658084-64-1Purity ≥98%

    Description: Daporinad (also known as APO866 and FK866) is a novel and potent inhibitor of nicotinamide phosphoribosyltransferase (NMPRTase) with IC50 of 0.09 nM in a cell-free assay. FK866 is a small molecule with potential antineoplastic and antiangiogenic activities. FK866binds to and inhibits nicotinamide phosphoribosyltransferase (NMPRTase), inhibiting the biosynthesis of nicotinamide adenine dinucleotide (NAD+) from niacinamide (vitamin B3), which may deplete energy reserves in metabolically active tumor cells and induce tumor cell apoptosis. In addition, this agent may inhibit tumor cell prioduction of vascular endothelial growth factor (VEGF), resulting in the inhibition of tumor angiogenesis. 

    References: Blood. 2009 Apr 2;113(14):3276-86; Arthritis Rheum. 2011 Jul;63(7):1866-77.

    Related CAS #: 201034-75-5; 658084-64-1;          

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    Molecular Weight (MW)391.51
    FormulaC24H29N3O2
    CAS No.658084-64-1
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 78 mg/mL (199.2 mM)
    Water: <1 mg/mL
    Ethanol: <1 mg/mL
    Solubility (In vivo)45% Propylene glycol (dissolve first)+5% Tween 80+ddH2O: 15mg/mL
    SynonymsAPO 866; FK 866; FK-866; Daporinad; APO866; APO-866; FK866; K 22.175; 


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    In Vitro

    In vitro activity: APO866 at low concentrations ranging from 0.09-27 nM induces dose-dependent cytotoxicity in 41 hematologic malignant cells including acute myeloid leukemia [AML], acute lymphoblastic leukemia [ALL], mantle cell lymphoma [MCL], chronic lymphocytic leukemia [CLL], and T-cell lymphoma. APO866 at low concentrations ranging from 0-10 nM induces cell death, this effect is independent of caspase activation but is associated with depolarization of mitochondrial membrane. APO866 at concentrations ranging from 0-10 nM dose-dependently induces depletion of intracellular NAD and ATP contents and cell death in various hematologic cancer cells. APO866 at concentration of 10 nM inhibits PBEF-induced secretion of MMP-3, CCL2, and CXCL8 in HFFF2 cells.


    Cell Assay: For MTT assays, 0.5 × 106 cells/mL is plated in triplicate on 96-well plates. APO866 (0.01 nM-100 nM) is added in 50 μL of culture medium, with culture medium alone serving as control. After 72 or 96 hours of incubation, 15 μL of dye solution is added to each well and cells are incubated for an additional 4 hours. Stop solution (100 μL/well) is added for 1 hour and the absorbance is read at 570 nm on a spectrophotometer. For trypan blue dye exclusion staining, 0.5 × 105 cells/well is grown in 6-well plates with 1 mL media in the absence or presence of APO866 for 96 hours. Cells from each sample are incubated with 10 μL trypan blue solution (at a 1:1 ratio [vol/vol] for 1 minute). Cell survival is determined by calculating proportion of live (unstained) cells.

    In VivoAPO866 administered intraperitoneally at dose of 20 mg/kg twice a day for 4 days, repeat weekly over 3 weeks, prevents and abrogats tumor growth in C.B.-17 SCID mice xenograft models of human AML, lymphoblastic lymphoma, and leukemia. APO866 at dose of 0.12 mg/kg/hour prevents joint destruction and leukocyte infiltration through inhibition of PBEF in mice with CIA.
    Animal modelC.B.-17 SCID mice xenograft models of human AML, lymphoblastic lymphoma, and leukemia.
    Formulation & DosageDissolved in 0.9% saline; 20 mg/kg; i.p. injection
    References

    Blood. 2009 Apr 2;113(14):3276-86; Arthritis Rheum. 2011 Jul;63(7):1866-77.


    These protocols are for reference only. InvivoChem does not independently validate these methods.

    FK866 (APO866, Daporinad)


    FK866 (APO866, Daporinad)

    APO866 induces time-dependent cell death in malignant cells from several hematologic malignancies. Blood. 2009 Apr 2;113(14):3276-86. 
     

    FK866 (APO866, Daporinad)

    APO866-induced cell death is independent of caspase activation, and is associated with depolarization of mitochondrial membrane.


    FK866 (APO866, Daporinad)

    APO866-mediated cell death involves autophagy. Blood. 2009 Apr 2;113(14):3276-86. 
     

    FK866 (APO866, Daporinad)

    APO866 induces depletion of intracellular NAD and ATP contents and cell death in various hematologic cancer cells, and extracellular addition of nicotinamide or NAD prevents APO866-mediated cell death. Blood. 2009 Apr 2;113(14):3276-86. 

    FK866 (APO866, Daporinad)

    In vivo antitumor activity of APO866 in mouse xenograft models of human leukemia and lymphoma. Blood. 2009 Apr 2;113(14):3276-86. 
     

    FK866 (APO866, Daporinad)

    In vivo pharmacokinetic and absence of toxicity effect of APO866 in mice. Blood. 2009 Apr 2;113(14):3276-86. 
     

    FK866 (APO866, Daporinad)


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