Epacadostat

CHF 160.00
In stock
AG-CR1-3634-M0055 mgCHF 160.00
AG-CR1-3634-M02525 mgCHF 580.00
More Information
Product Details
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
  • 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
  1. 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)
  2. Selective inhibition of IDO1 effectively regulates mediators of antitumor immunity: X. Liu, et al.; Blood 115, 3520 (2010)
  3. Trial watch: IDO inhibitors in cancer therapy: E. Vacchelli, et al.; Oncoimmunology 3, e957994 (2014)
  4. Challenges in the Discovery of Indoleamine 2,3-Dioxygenase 1 (IDO1) Inhibitors: U.F. Roehrig, et al.; J. Med. Chem. 58, 9421 (2015)
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