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.