Epacadostat
Code | Size | Price |
---|
AG-CR1-3634-M005 | 5 mg | £120.00 |
Quantity:
AG-CR1-3634-M025 | 25 mg | £410.00 |
Quantity:
Prices exclude any Taxes / VAT
Overview
Regulatory Status: RUO
Shipping:
-20°C
Storage:
Short Tem: +4°C, Long Term: -20°C
Images
Documents
Further Information
Alternate Names/Synonyms:
INCB24360; (E)-N?-(3-Bromo-4-fluorophenyl)-N-hydroxy-4-((2-(sulfamoylamino-1,2,5-oxadiazole-3-carboxamide)
Appearance:
White to off-white solid.
CAS:
1204669-58-8
EClass:
32160000
Form (Short):
liquid
Handling Advice:
Keep cool and dry.Keep under inert gas.Protect from light.
InChi:
InChI=1S/C11H13BrFN7O4S/c12-7-5-6(1-2-8(7)13)17-11(18-21)9-10(20-24-19-9)15-3-4-16-25(14,22)23/h1-2,5,16,21H,3-4H2,(H,15,20)(H,17,18)(H2,14,22,23)
InChiKey:
FBKMWOJEPMPVTQ-UHFFFAOYSA-N
Long Description:
Chemical. CAS: 1204669-58-8. Formula: C11H13BrFN7O4S. MW: 438.2. Potent and selective competitive indoleamine 2,3-dioxygenase (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).
MDL:
MFCD29075639
Molecular Formula:
C11H13BrFN7O4S
Molecular Weight:
438.2
Package Type:
Vial
Product 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).
Purity:
>98% (HPLC)
SMILES:
O=S(NCCNC1=NON=C1/C(NC2=CC=C(F)C(Br)=C2)=N/O)(N)=O
Solubility Chemicals:
Soluble in DMSO (~30mg/ml). Insoluble in water.
Transportation:
Non-hazardous
UNSPSC Category:
Biochemical Reagents
UNSPSC Number:
12352200
Use & Stability:
Stable for at least 2 years after receipt when stored at -20°C.
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)
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