Molecular Formula | C9H7ClFN5O2 |
Molar Mass | 271.64 |
Density | 1.78±0.1 g/cm3(Predicted) |
Boling Point | 504.7±60.0 °C(Predicted) |
Appearance | Solid |
pKa | 7.54±0.69(Predicted) |
Storage Condition | -20℃ |
In vitro study | In HeLa cells, INCB024360 showed high inhibitory activity against IDO1 with an IC50 of 19 nM. In the co-culture system of dendritic cells or tumor cells of human allogeneic lymphocytes, INCB024360, through IDO1 inhibition, reverses IDO-expressed HeLa cells or DCs-mediated T cell inhibition, and increases the differentiation and functional activity of CD4 T cells, CD8 T cells, and NK cells. |
In vivo study | In mice bearing GM-CSF-secretory B16 tumors, INCB024360 (75 mg/kg B. I. d) caused a dose-dependent inhibition of tumor growth. INCB024360 significantly inhibited tumor growth in immunocompetent mice, but had no inhibitory effect on immunodeficient mice. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 3.681 ml | 18.407 ml | 36.813 ml |
5 mM | 0.736 ml | 3.681 ml | 7.363 ml |
10 mM | 0.368 ml | 1.841 ml | 3.681 ml |
5 mM | 0.074 ml | 0.368 ml | 0.736 ml |
biological activity | INCB024360 is a potent, competitive, its IC50 is 67 nM. Phase 2. INCB024360 analog (INCB14943) is a potent competitive inhibitor of IDO1 (indoleamine-(2,3)-dioxygenase) with an IC50 of 67 nM. |
Target | Value |
IDO1 (Cell-free assay) | 67 nM |