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    INCB024360 analogue
    INCB024360 analogue

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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 #: V0940
    CAS #: 914471-09-3Purity ≥98%

    Description: INCB024360 analogue (formerly known as IDO-IN-2) is a potent, orally available hydroxyamidine, competitive inhibitor of IDO1 (indoleamine-(2,3)-dioxygenase) with IC50 of 67 nM. INCB024360 analog has potential immunomodulating and antineoplastic activities. In vivo testing of INCB024360 analog in mice demonstrated pharmacodynamic inhibition of IDO, as measured by decreased kynurenine levels (>50%) in plasma and dose dependent efficacy. 

    References: J Med Chem. 2009 Dec 10;52(23):7364-7; Blood. 2010 Apr 29;115(17):3520-30.

    Related CAS:1204669-58-8 or 1204669-37-3 (INCB024360)

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    Molecular Weight (MW)271.64
    FormulaC9H7ClFN5O2
    CAS No.914471-09-3
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 54 mg/mL (198.8 mM)
    Water: <1 mg/mL
    Ethanol: 54 mg/mL (198.8 mM)
    Solubility (In vivo)2% DMSO+corn oil: 5mg/mL 
    SynonymsIDO-IN-2;INCB024360 analog; INCB24360 analog; Epacadostat analog
    SMILES CodeO/N=C(C1=NON=C1N)/NC2=CC=C(F)C(Cl)=C2


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    In Vitro

    In vitro activity: In HeLa cells, INCB024360 shows higher inhibitory activity on IDO1 with IC50 of 19 NM. In coculture systems of human allogeneic lymphocytes with dendritic cells or tumor cells, INCB024360, via IDO1 inhibition, reverses T-cell suppression mediated by IDO-expressing HeLa cells or DCs, and increases the proliferation and functional activity of CD4+ T cells, CD8+ T cells, and NK cells.


    Kinase Assay: Human IDO with an N-terminal His tag was expressed in E.coli and purified to homogeneity. IDO catalyzed the oxidative cleavage of the pyrrole ring of the indole nucleus of tryptophan to yield N’-formylkynurenine. The assays were performed at room temperature using 20 nM IDO and 2 mM D-Trp in the presence of 20 mM ascorbate, 3.5 μM methylene blue and 0.2 mg/mL catalase in 50 mM potassium phosphate buffer (pH 6.5). The initial reaction rates were recorded by continuously following the absorbance increase at 321 nm due to the formation of N’-formlylkynurenine.


    Cell Assay: In Hela cells, INCB024360 analogue selectively inhibited the activity of human IDO1 with an IC50 value of 19 nM. In murine B16 cells, INCB024360 analogue inhibited IDO with an IC50 value of 46 NM.

    In VivoIn mice bearing GM-CSF-secreting B16 tumors, INCB024360 (75 mg/kg b.i.d) causes dose dependent inhibition of tumor growth. INCB024360 significantly suppresses tumor growth in immunocompetent, but not immunodeficient, mice.
    Animal modelMice bearing GM-CSF-secreting B16 tumors
    Formulation & DosageDissolved in 5% DMA, 47.5% propylene glycol; 75 mg/kg; s.c. administration
    References

    J Med Chem. 2009 Dec 10;52(23):7364-7; Blood. 2010 Apr 29;115(17):3520-30.


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

    INCB024360 analogue

    INCB024360 potently inhibits kynurenine production in IFN-γ–treated human HeLa cells. Blood. 2010 Apr 29;115(17):3520-30. 
     

    INCB024360 analogue

    IDO1 inhibition reverses T-cell suppression mediated by IDO-expressing HeLa cells or DCs. Blood. 2010 Apr 29;115(17):3520-30. 
     

    INCB024360 analogue

    IDO1 inhibition increases the proliferation and functional activity of CD4+ T cells, CD8+ T cells, and NK cells. Blood. 2010 Apr 29;115(17):3520-30.  
     

    INCB024360 analogue

    IDO1 inhibition reduces the conversion of CD4+Foxp3− T cells to CD4+Foxp3+ Treg-like cells. Blood. 2010 Apr 29;115(17):3520-30.
     

    INCB024360 analogue

    IDO1 inhibition suppresses tumor growth in immunocompetent, but not immunodeficient, mice. Blood. 2010 Apr 29;115(17):3520-30. 


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