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Numidargistat (CB-1158) dihydrochloride is a potent and orally active inhibitor of arginase , with IC 50 s of 86 nM and 296 nM for recombinant human arginase 1 and recombinant human arginase 2 , respectively. Immuno-oncology agent.
IC50& Target:IC50: 86 nM (Arginase 1), 296 nM (Arginase 2)
In Vitro:Numidargistat dihydrochloride is a potent and orally-bioavailable inhibitor of arginase, with IC 50 s of 86 and 296 nM for recombinant human arginase 1 and 2, respectively. Numidargistat dihydrochloride inhibits native rginase 1 (Arg1) in human granulocyt
In Vivo:Numidargistat dihydrochloride (100mg/kg, p.o., twice per day) increases the number of tumor-infiltrating cytotoxic cells and decreases myeloid cells in mice. Numidargistat dihydrochloride in combination with PD-L1 blockade or LY 188011 inhibits tumor gro
Biological Activity:Numidargistat (CB-1158) dihydrochloride is a potent and orally active inhibitor of arginase , with IC 50 s of 86 nM and 296 nM for recombinant human arginase 1 and recombinant human arginase 2 , respectively. Immuno-oncology agent.