CB-1158 dihydrochloride is an effective and orally active inhibitor of arginase (IC50s: 86 nM and 296 nM for recombinant human arginase 1 and 2).

CB-1158 inhibits native arginase 1 (Arg1) in human granulocyte, erythrocyte, and hepatocyte lysate (IC50s: 178 nM, 116 nM, and 158 nM), and blocks Arg1 in cancer patient plasma (IC50: 122 nM). CB-1158 also exhibits potent inhibitory activity against arginase in human HepG2, K562 cell lines, and primary human hepatocytes (IC50s: 32, 139, 210 μM). CB-1158 shows no effect on NOS and not directly cytotoxic to murine cancer cell lines.

CB-1158 (100 mg/kg, p.o., twice per day) decreases the number of myeloid cells and increases tumor-infiltrating cytotoxic cells in mice. CB-1158 in combination with LY 188011 inhibits tumor growth in mice bearing CT26 cancer cells.

T10692

C11H24BCl2N3O5

360.04

CB-1158 dihydrochloride;INCB01158 dihydrochloride;CB-1158 dihydrochloride (2095732-06-0 free base)

H2O:50 mg/mL (138.87 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years