INCB024360 analog

INCB024360 analog is a potent IDO1 inhibitor that demonstrates IC₅₀ values of 67 and 19 nM for human IDO in enzymatic activity and HeLa cell assays, respectively.^1,2,3 It is inactive against tryptophan 2,3-dioxygenase (IC₅₀ > 10 µM).² At 25-75 mg/kg, subcutaneous administration of INCB024360 analog to mice significantly decreased kynurenine levels in plasma and dose-dependently reduced the growth of GM-CSF-secreting B16 tumor xenografts.² A fluorine-18 moiety has been used to label this compound for use as a probe for imaging IDO1 expression via positron emission tomography.⁴

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1. Liu, X., Shin, N., Koblish, H.K., et al. Selective inhibition of IDO1 effectively regulates mediators of antitumor immunity. Blood 115(17), 3520-3530 (2010).

2. Yue, E.W., Douty, B., Wayland, B., et al. Discovery of potent competitive inhibitors of indoleamine 2,3-dioxygenase with in vivo pharmacodynamic activity and efficacy in a mouse melanoma model. J. Med. Chem. 52(23), 7364-7367 (2009).

3. Tomek, P., Palmer, B.D., Flanagan, J.U., et al. Formation of an N-formylkynurenine-derived fluorophore and its use for measuring indoleamine 2,3-dioxygenase 1 activity. Anal. Bioanal. Chem. 405(8), 2515-2524 (2013).

4. Huang, X., Gillies, R.J., and Tian, H. Synthesis of [18 F] 4-amino-N-(3-chloro-4-fluorophenyl)-N'-hydroxy-1,2,5-oxadiazole-3-carboximidamide (IDO5L): A novel potential PET probe for imaging of IDO1 expression. J. Labelled Comp. Radiopharm. 58(4), 156-162 (2015).