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.
CAS Number: 1204669-58-8
Molecular Weight: 438.23
Chemical Name: (Z)-N-(3-bromo-4-fluorophenyl)-N'-hydroxy-4-(2-(sulfamoylamino)ethylamino)-1, 2, 5-oxadiazole-3-carboximidamide
Appearance: Solid Power.
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO up to 100 mM
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥360 days if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined.
HS Tariff Code: 382200
How to use
INCB024360 was used at 1 µM final concentration in various in vitro assays.
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.
- 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.
- Liu X, et al. Selective inhibition of IDO1 effectively regulates mediators of antitumor immunity. (2010) Blood. 115(17):3520-30.
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