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    Epacadostat (INCB024360)
    Epacadostat (INCB024360)

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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 #: V0942
    CAS #: 1204669-58-8 Purity ≥98%

    Description: Epacadostat (formerly known as INCB024360 or INCB24360) is an orally available, potent and selective IDO1 inhibitor with IC50 of 10 nM. Epacadostat has potential immunomodulating and antineoplastic activities. By inhibiting IDO1 and decreasing kynurenine in tumor cells, Epacadostat increases and restores the proliferation and activation of various immune cells, including dendritic cells, NK cells, T-cells, and a reduction in tumor-associated regulatory T cells. Epacadostat was under investigation in a phase 3 clinical trial. But according to the results presented at the 2018 ASCO Annual Meeting, in patients with unresectable or metastatic melanoma, adding epacadostat to pembrolizumab (Keytruda) did not result in greater clinical benefit over pembrolizumab alone, according to data from the phase III ECHO-301/KEYNOTE-252 study. 

    References: Blood. 2010 Apr 29;115(17):3520-30; Mol Cancer Ther. 2010 Feb;9(2):489-98.

    Related CAS #: or 1204669-37-3 (INCB024360), 914471-09-3 (INCB024360 analog) 

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    Molecular Weight (MW)438.23
    FormulaC11H13BrFN7O4S
    CAS No.1204669-58-8; 1204669-37-3 (INCB024360); 
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 87 mg/mL (198.5 mM)
    Water: <1 mg/mL
    Ethanol: 53 mg/mL (120.9 mM)
    Solubility (In vivo)10%DMSO+90%PEG400: 30mg/mL
    SynonymsINCB024360 or INCB24360;Epacadostat-analog; IDO-IN-1; INCB 024360; INCB-024360; INCB-24360; INCB 24360;
    SMILES CodO=S(NCCNC1=NON=C1/C(NC2=CC=C(F)C(Br)=C2)=N/O)(N)=O


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    In Vitro

    In vitro activity: Epacadostat (formerly known as INCB024360 or INCB24360) is an orally available, potent and selective IDO1 inhibitor with IC50 of 10 nM. Epacadostat has potential immunomodulating and antineoplastic activities. By inhibiting IDO1 and decreasing kynurenine in tumor cells, Epacadostat increases and restores the proliferation and activation of various immune cells, including dendritic cells, NK cells, T-cells, and a reduction in tumor-associated regulatory T cells. Epacadostat was under investigation in a phase 3 clinical trial. But according to the results presented at the 2018 ASCO Annual Meeting, in patients with unresectable or metastatic melanoma, adding epacadostat to pembrolizumab (Keytruda) did not result in greater clinical benefit over pembrolizumab alone, according to data from the phase III ECHO-301/KEYNOTE-252 study. In IFN-γ–treated human HeLa cells, INCB024360 potently inhibits kynurenine production. INCB024360 also promotes T and natural killer (NK)-cell growth, increases IFN-gamma production, and reduces conversion to regulatory T (T(reg))-like cells. 


    Kinase Assay: Epacadostat (formerly known as INCB024360 or INCB24360) is an orally available, potent and selective IDO1 inhibitor with IC50 of 10 nM. 


    Cell Assay: In Hela cells, INCB024360 selectively inhibits the activity of human IDO1 with IC50 values of about 10nM. On the other hand INCB024360demonstrates little inhibition activity against human IDO1 or TDO (tryptophan 2, 3-dioxygenase). In coculture systems of human dendritic cells with allogeneic lymphocytes, INCB024360 inhibit T-cell proliferation and cytokine production and influence the viability of NK cells. INCB024360 also increase CD86 expression and promote activation T cells by DCs. 

    In VivoINCB024360 (100 mg/kg, p.o.), via IDO1 inhibition, suppresses kyn generation and tumor growth in immunocompetent, but not immunodeficient, mice. In mice bearing CT26 colon carcinoma, INCB024360 (100 mg/kg, p.o.) also inhibits the growth of IDO-expressing tumors by reducing kynurenine.
    Animal modelFemale C57BL/6 or Balb/c nu/nu mice bearing PAN02 pancreatic tumors
    Formulation & DosageDissolved in  3% N,N–Dimethylacetamide, 10% (2-Hydroxypropyl) β-Cyclodextrin; 100 mg/kg; p.o. administration
    ReferencesBlood. 2010 Apr 29;115(17):3520-30; Mol Cancer Ther. 2010 Feb;9(2):489-98


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

    Epacadostat (INCB024360)

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

    Epacadostat (INCB024360)

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

     


    Epacadostat (INCB024360)

    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.

    Epacadostat (INCB024360)

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

    Epacadostat (INCB024360)

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


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