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- 详细信息
- 文献和实验
- 技术资料
- 保存条件：
-20°C, stored under nitrogen, away from moisture
- 英文名：
CB-1158 dihydrochloride; INCB01158 dihydrochloride
- 库存：
货期：1-2天
- 供应商：
MedChemExpress LLC
- 规格：
10 mM * 1 mL/5 mg/10 mg/25 mg
| 规格： | 10 mM * 1 mL | 产品价格： | ￥2750.0 |
|---|---|---|---|
| 规格： | 5 mg | 产品价格： | ￥2500.0 |
| 规格： | 10 mg | 产品价格： | ￥4500.0 |
| 规格： | 25 mg | 产品价格： | ￥9500.0 |
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Numidargistat dihydrochloride
MCE 国际站：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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