Epacadostat | IDO1 inhibitor
NMR (Conforms)
Available Options
| Size: | Price | Quantity | |
|---|---|---|---|
| 5 mg | $45.00 | ||
| 25 mg | $150.00 |
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. 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 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
NMR (Conforms)
Safety Data Sheet:
Product Data Sheet:
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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. 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 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
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