Epacadostat | IDO1 inhibitor

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
Stability:
Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.
Shipping Code:
RT

Available Options

Size:PriceQuantity 
5 mg$45.00
25 mg$150.00
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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.4-6

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. 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 37762
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

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
Stability:
Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.
Shipping Code:
RT

Safety Data Sheet:

N/A

Product Data Sheet:

Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications. Please note that we do not sell to individuals and that all orders placed by non-research organizations will incur a $20 restocking/refund fee

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