| Storage: | Powder:4oC 1 year. DMSO:4oC3 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 potentand selective indoleamine 2,3-dioxygenase (IDO1) inhibitor with IC50~10 nM It displays high selectivity over other related enzymes such as IDO2 ortryptophan 2,3-dioxygenase (TDO). In coculture systems of human allogeneiclymphocytes with dendritic cells (DCs) or tumor cells, INCB024360 inhibition ofIDO1 promotes T and natural killer (NK)-cell growth, increases IFN-gammaproduction, and reduces conversion to regulatory T (T(reg))-like cells. Administration of INCB024360 totumor-bearing mice significantly inhibits tumor growth in alymphocyte-dependent manner. INCB024360has completed Phase I clinical trials and is now being used in combination withother cancer immunotherapy agents.
How to Use:
In vitro: INCB024360was 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.YueEW, et al. Discovery of potent competitive inhibitors of indoleamine2,3-dioxygenase with in vivo pharmacodynamic activity and efficacy in a mousemelanoma model. (2009) J Med Chem. 52(23):7364-7.
- 2. LiuX, et al. Selective inhibition of IDO1 effectively regulates mediators ofantitumor immunity. (2010) Blood. 115(17):3520-30.
INCB024360_spec.pdf
INCB024360_MSDS.pdf
Products are for research use only. Not for human use.
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