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Numidargistat

CAS No. : 2095732-06-0

產品活性：Numidargistat (CB-1158) is a potent and orally active inhibitor of arginase, with IC₅₀s of 86 nM and 296 nM for recombinant human arginase 1 and recombinant human arginase 2, respectively. Immuno-oncology agent.

研究領域：Immunology/Inflammation  |  Metabolic Enzyme/Protease

作用靶點：Arginase

In Vitro: Numidargistat is a potent and orally-bioavailable inhibitor of arginase, with IC₅₀s of 86 and 296 nM for recombinant human arginase 1 and 2, respectively. Numidargistat inhibits native rginase 1 (Arg1) in human granulocyte, erythrocyte, and hepatocyte lysate with IC₅₀s of 178 nM, 116 nM and 158 nM, respectively, and blocks Arg1 in cancer patient plasma (IC₅₀, 122 nM). Numidargistat also exhibits potent inhibitory activity against arginase in human HepG2, K562 cell lines and primary human hepatocytes with IC₅₀s of 32, 139, 210 μM, respectively. Numidargistat show no effect on NOS. In addition, Numidargistat is not directly cytotoxic to murine cancer cell lines.

In Vivo: Numidargistat (100 mg/kg, p.o., twice per day) increases the number of tumor-infiltrating cytotoxic cells and decreases myeloid cells in mice. Numidargistat in combination with PD-L1 blockade or gemcitabine inhibits tumor growth in mice bearing CT26 cancer cells.

相關產品：Covalent Screening Library Plus  |  Bioactive Compound Library Plus  |  Immunology/Inflammation Compound Library  |  Metabolism/Protease Compound Library  |  Anti-Cancer Compound Library  |  Small Molecule Immuno-Oncology Compound Library  |  Covalent Screening Library  |  Orally Active Compound Library  |  Anti-Cancer Metabolism Compound Library  |  Heterocyclic Compound Library  |  Broussonin E  |  Numidargistat dihydrochloride  |  Arginase inhibitor 1  |  nor-NOHA acetate  |  BEC hydrochloride  |  DL-Norvaline  |  Piceatannol 3'-O-glucoside  |  ARG1-IN-1  |  2-Aminoimidazole  |  ABH hydrochloride

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