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INCB024360

(CAS No:914471-09-3)
INCB024360 analogue is a potent, competitive IDO1 (indoleamine-(2,3)-dioxygenase) inhibitor with IC50 of 67 nM. Phase 2.
CAS No:914471-09-3
Molecular Weight(MW):271.64
Purity:99.00%
Specification:500MG;1G;5G;10G;50G;100G
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QC Documents
　COA 　MSDS 　HPLC 　NMR
ChemicalInfomation
CAS No: 914471-09-3
Molecular formula(MF) C9H7ClFN5O2
Molecular Weight(MW): 271.64
Alias
Solubility
In vitro DMSO 54 mg/mL warmed (198.79 mM)
Ethanol 54 mg/mL warmed (198.79 mM)
Water <1 mg/mL
In vivo 5% DMSO+45% PEG 300+ddH2O 22mg/mL
Biological Activity
Description INCB024360 analogue is a potent, competitive IDO1 (indoleamine-(2,3)-dioxygenase) inhibitor with IC50 of 67 nM. Phase 2.
Targets
IDO1 [1]
67 nM
In vitro

In HeLa cells, INCB024360 shows higher inhibitory activity on IDO1 with IC50 of 19 nM. [1] In coculture systems of human allogeneic lymphocytes with dendritic cells or tumor cells, INCB024360, via IDO1 inhibition, reverses T-cell suppression mediated by IDO-expressing HeLa cells or DCs, and increases the proliferation and functional activity of CD4+ T cells, CD8+ T cells, and NK cells. [2]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human HeLa cells Function assay Inhibition of indoleamine 2,3-dioxygenase in IFN-gamma-stimulated human HeLa cells assessed as kynurenine formation by spectrophotometry, IC50=19 nM 19507862
mouse B16 cells Function assay Inhibition of indoleamine 2,3-dioxygenase in mouse B16 cells assessed as kynurenine formation by spectrophotometry, IC50=46 nM 19507862
mouse P815B clone-6 cells Function assay Inhibition of human IDO1 transfected in mouse P815B clone-6 cells by HPLC analysis, IC50=60 nM 22616902
P815 clone 6 cells Function assay Inhibition of mouse IDO1 in P815 clone 6 cells by HPLC analysis, IC50=0.1 μM 22616902
HEK293 clone 6 cells Function assay Inhibition of human IDO1 transfected in HEK293 clone 6 cells by HPLC analysis 22616902

... Click to View More Cell Line Experimental Data
In vivo In mice bearing GM-CSF-secreting B16 tumors, INCB024360 (75 mg/kg b.i.d) causes dose dependent inhibition of tumor growth. [1] INCB024360 significantly suppresses tumor growth in immunocompetent, but not immunodeficient, mice. [2]
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