150 CHF CHF 150.00
AG-CR1-3634-M0055 mgCHF 150.00
AG-CR1-3634-M02525 mgCHF 530.00
|Purity Chemicals||≥98% (HPLC)|
|Appearance||White to off-white solid.|
|Solubility||Soluble in DMSO (~30mg/ml). Insoluble in water.|
|Shipping and Handling|
|Short Term Storage||+4°C|
|Long Term Storage||-20°C|
Keep cool and dry.
Keep under inert gas.
Protect from light.
|Use/Stability||Stable for at least 2 years after receipt when stored at -20°C.|
|Product Specification Sheet|
- Potent and selective competitive indoleamine 2,3-dioxygenase 1 (IDO1) inhibitor. Inhibits IDO1 in enzymatic (IC50=72nM) and in cellular tests (IC50=7.1nM), suppresses tryptophan catabolism in vivo and impedes tumor growth. Displays high selectivity over other related enzymes such as IDO2 or tryptophan 2,3-dioxygenase (TDO).
- Exhibits potent in vitro and in vivo immunomodulating and antineoplastic activities.
- By inhibiting IDO1 and decreasing kynurenine levels in tumor cells, Epacadostat increases and restores the proliferation and activation of various immune cells, including dendritic cells (DCs), NK cells and T-lymphocytes, as well as interferon (IFN) production and reduces tumor-associated regulatory T cells (Tregs).
- Hydroxyamidine inhibitors of indoleamine-2,3-dioxygenase potently suppress systemic tryptophan catabolism and the growth of IDO-expressing tumors: H.K. Koblish, et al.; Mol. Cancer Ther. 9, 489 (2010)
- Selective inhibition of IDO1 effectively regulates mediators of antitumor immunity: X. Liu, et al.; Blood 115, 3520 (2010)
- Trial watch: IDO inhibitors in cancer therapy: E. Vacchelli, et al.; Oncoimmunology 3, e957994 (2014)
- Challenges in the Discovery of Indoleamine 2,3-Dioxygenase 1 (IDO1) Inhibitors: U.F. Roehrig, et al.; J. Med. Chem. 58, 9421 (2015)