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AdipoGen Life Sciences
Epacadostat
150
CHF
CHF 150.00
In stock
AG-CR1-3634-M0055 mgCHF 150.00
AG-CR1-3634-M02525 mgCHF 530.00
Product Details | |
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Synonyms | INCB24360; (E)-N’-(3-Bromo-4-fluorophenyl)-N-hydroxy-4-((2-(sulfamoylamino-1,2,5-oxadiazole-3-carboxamide) |
Product Type | Chemical |
Properties | |
Formula |
C11H13BrFN7O4S |
MW | 438.2 |
CAS | 1204669-58-8 |
Purity Chemicals | ≥98% (HPLC) |
Appearance | White to off-white solid. |
Solubility | Soluble in DMSO (~30mg/ml). Insoluble in water. |
InChi Key | FBKMWOJEPMPVTQ-UHFFFAOYSA-N |
Smiles | O=S(NCCNC1=NON=C1/C(NC2=CC=C(F)C(Br)=C2)=N/O)(N)=O |
Shipping and Handling | |
Shipping | AMBIENT |
Short Term Storage | +4°C |
Long Term Storage | -20°C |
Handling Advice |
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. |
Documents | |
MSDS | Download PDF |
Product Specification Sheet | |
Datasheet | Download PDF |
Description
- 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).
Product References
- 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)
- Inhibition of STAT-mediated cytokine responses to chemically-induced colitis prevents inflammation-associated neurobehavioral impairments: R. Sin, et al.; Brain Behav. Immun. 114, 173 (2023)