INCB024360(Epacadostat),IDOInhibitor

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. 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. 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.

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