Epacadostat (INCB024360) analogue

Catalog No.S7587 Batch:S758701

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Technical Data

Formula

C9H7ClFN5O2
Molecular Weight 271.64 CAS No. 914471-09-3
Solubility (25°C)* In vitro DMSO 54 mg/mL (198.79 mM)
Ethanol 54 mg/mL (198.79 mM)
Water Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description Epacadostat (INCB024360) analogue (INCB14943) is a potent, competitive IDO1 (indoleamine-(2,3)-dioxygenase) inhibitor with IC50 of 67 nM.
Targets
IDO1 [1]
(Cell-free assay)
67 nM
In vitro

In HeLa cells, INCB024360 shows higher inhibitory activity on IDO1 with IC50 of 19 nM. [1] 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. [2]
In vivo

In mice bearing GM-CSF-secreting B16 tumors, INCB024360 (75 mg/kg b.i.d) causes dose dependent inhibition of tumor growth. [1] INCB024360 significantly suppresses tumor growth in immunocompetent, but not immunodeficient, mice. [2]

Protocol (from reference)

Animal Study:

[1]
  • Animal Models

    Mice bearing GM-CSF-secreting B16 tumors

  • Dosages

    75 mg/kg b.i.d

  • Administration

    s.c.

Selleck's Epacadostat (INCB024360) analogue has been cited by 3 publications

IDO1 inhibitors are synergistic with CXCL10 agonists in inhibiting colon cancer growth [ Biomed Pharmacother, 2024, 179:117412] PubMed: 39255734
Granulocytic myeloid-derived suppressor cells increase infection risk via the IDO/IL-10 pathway in patients with hepatitis B virus-related liver failure [ Front Immunol, 2022, 13:966514] PubMed: 36685516
[ Oncoimmunology, 2017, ] PubMed: 29209565

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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