| Storage: | Powder: 4oC 1 year. DMSO: 4oC 3 month; -20oC 1 year. |
| Chemical Name: | (E)-N'-(3-bromo-4-fluorophenyl)-N-hydroxy-4-((2-(sulfamoylamino)ethyl)amino)-1,2,5-oxadiazole-3-carboximidamide |
| Solubility: | DMSO up to 100 mM |
| CAS#: | 1204669-58-8 |
| Purity: | ≥98% |
| Formula: | C11H13BrFN7O4S |
| Molecular Weight: | 438.23 |
Biological Activity:
INCB024360 is a potent and selective indoleamine 2,3-dioxygenase (IDO1) inhibitor with IC50 ~10 nM It displays high selectivity over other related enzymes such as IDO2 or tryptophan 2,3-dioxygenase (TDO). In coculture systems of human allogeneic lymphocytes with dendritic cells (DCs) or tumor cells, INCB024360 inhibition of IDO1 promotes T and natural killer (NK)-cell growth, increases IFN-gamma production, and reduces conversion to regulatory T (T(reg))-like cells. Administration of INCB024360 to tumor-bearing mice significantly inhibits tumor growth in a lymphocyte-dependent manner. INCB024360 has completed Phase I clinical trials and is now being used in combination with other cancer immunotherapy agents.
How to Use:
In vitro: INCB024360 was used at 1 µM final concentration in various in vitro assays.
In vivo: INCB024360 was dosed at 75 mg/Kg (BID, subcutaneous injection) to mice bearing GM-CSF-secreting B16 tumors. Formulation is 5% DMA, 47.5% propylene glycol.
References:
- 1. Yue EW, et al. Discovery of potent competitive inhibitors of indoleamine 2,3-dioxygenase with in vivo pharmacodynamic activity and efficacy in a mouse melanoma model. (2009) J Med Chem. 52(23):7364-7.
- 2. Liu X, et al. Selective inhibition of IDO1 effectively regulates mediators of antitumor immunity. (2010) Blood. 115(17):3520-30.
Products are for research use only. Not for human use.
