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Numidargistat dihydrochloride

CAS No. :

MCE 站：Numidargistat dihydrochloride

产品活性：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。

研究领域：Immunology/Inflammation  |  Metabolic Enzyme/Protease

作用靶点：Arginase

In Vitro: Numidargistat dihydrochloride 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 dihydrochloride 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 dihydrochloride 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 dihydrochloride shows no effect on NOS. In addition, Numidargistat dihydrochloride is not directly cytotoxic to murine cancer cell lines.

In Vivo: 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.

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