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Epacadostat | IDO1 inhibitor

Epacadostat (1204669-58-8) is a potent (IC50 = 10nM)1 and selective inhibitor of Indoleamine-2,3-dioxygenase 1 (IDO1) with no activity at IDO2 or TDO.2 It restored tryptophan levels and significantly impaired kynurenine generation in CT26 colon carcinoma (IC50 = 76 nM) and PAN02 pancreatic carcinoma (IC50 = 27 nM) cells. Epacadostat increases the number and activity of tumor-infiltrating lymphocytes as well as increasing the ratio of effector T cells to regulatory T cells.1,2 Because of these immune system enhancing properties3, it is being investigated as a synergistic agent for use with other immuno-oncology agents such as anti-PD-1 and anti-CTL4 antibodies.4,5,6

References/Citations

1) Liu et al. (2010), Selective inhibition of IDO1 effectively regulates mediators of antitumor immunity; Blood 115 3520
2) Koblish et al. (2010), Hydroxyamidine Inhibitors of Indolamine-2,3-dioxygenase Potently Suppress Systemic Tryptophan Catabolism and the Growth of IDO-Expressing Tumors; Mol. Cancer Ther. 9 489
3) Jochems et al. (2016), The IDO1 selective inhibitor epacadostat enhances dendritic cell immunogenicity and lytic ability of tumor antigen-specific T cells; Oncotarget 7 3776
4) Yentz and Smith (2018), Indoleamine-2,3-dioxygenase Inhibition as a Strategy to Augment Cancer Immunotherapy; BioDrugs 32 311
5) Zhu  et al. (2019), Indoleamine Dioxygenase Inhibitors: Clinical Rationale and Current Development; Curr. Oncol. Rep. 21 2
6) Mitchell et al. (2018), Epacadostat Plus Pembrolizumab in Patients with Advanced Solid Tumors: Phase I Results From a Multicenter, Open-Label Phase I/II Trial (ECHO-202/KEYNOTE-037); J. Clin. Oncol. 36 3223

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Catalog#  10-4499-0005

$60.00
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CAS:
1204669-58-8
Catalog Number:
10-4499
Activity:
IDO1 inhibitor/ Cancer immunotherapy enhancer
Chemical Name:
N-(3-Bromo-4-fluorophenyl)-N’-hydroxy-4-{[2-(sulfamoylamino)ethyl]amino}-1,2,5-oxadiazole-3-carboximidamide
Alternate Name:
INCB024360
Molecular Weight:
438.23
Molecular Formula:
C11H13BrFN7O4S
Solubility:
Soluble in DMSO (up to at least 25 mg/ml)
Physical Properties:
White solid
Purity:
98% by HPLC
NMR (Conforms)
Storage Temperature:
-20°C (des.)
Stability:
Stable for 1 year as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.
Shipping Code:
RT
Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications.

Focus BiomoleculesPlymouth Meeting, PA USA1-855-FOCUS21

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