Numidargistat (CB-1158) dihydrochloride 是一种有效的，具有口服活性的精氨酸酶 (Arginase) 抑制剂，对重组人Arginase 1和Arginase 2的IC50值分别为 86 nM 和 296 nM。免疫肿瘤剂。

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 [1].

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 granulocyte, erythrocyte, and hepatocyte lysate with IC 50 s of 178 nM, 116 nM and 158 nM, respectively, and blocks Arg1 in cancer patient plasma (IC 50, 122 nM). Numidargistat dihydrochloride also exhibits potent inhibitory activity against arginase in human HepG2, K562 cell lines and primary human hepatocytes with IC 50 s of 32, 139, 210 μM, respectively. Numidargistat dihydrochloride shows no effect on NOS. In addition, Numidargistat dihydrochloride is not directly cytotoxic to murine cancer cell lines [1].

Numidargistat dihydrochloride (100 mg/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 growth in mice bearing CT26 cancer cells [1].

C11H24BCl2N3O5

360.04

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years