7ACC-2
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- CAS号:
- 1472624-85-3
- 英文名:
- 7ACC-2
- 英文别名:
- 7ACC2;7ACC-2;7ACC 2;7ACC 2; 7ACC-2; 7ACC 2; 7ACC-2;7-[benzyl(methyl)amino]-2-oxochromene-3-carboxylic acid;7-[Benzyl(methyl)amino]-2-oxo-2H-chromene-3-carboxylic acid;2H-1-Benzopyran-3-carboxylic acid, 7-[methyl(phenylmethyl)amino]-2-oxo-;7ACC2,MPC,MCT1,7ACC-2,Monocarboxylate Transporter,Inhibitor,lactate,pyruvate,Mitochondrial Metabolism,radiosensitizes,antitumor,mitochondrial,inhibit
- 中文名:
- 7ACC-2
- 中文别名:
- MCT抑制剂(7ACC2);7-[苄基(甲基)氨基]-2-氧代-2H-苯并吡喃-3-羧酸
- CBNumber:
- CB22729349
- 分子式:
- C18H15NO4
- 分子量:
- 309.32
- MOL File:
- 1472624-85-3.mol
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7ACC-2化学性质
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沸点:
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548.9±50.0 °C(Predicted)
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密度:
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1.368±0.06 g/cm3(Predicted)
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储存条件:
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2-8°C
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溶解度:
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insoluble in EtOH; insoluble in H2O; ≥47.5 mg/mL in DMSO
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形态:
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Powder
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酸度系数(pKa):
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-98.37±0.20(Predicted)
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颜色:
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Light yellow to yellow
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7ACC-2性质、用途与生产工艺
7ACC2是一种有效的MCT1抑制剂,在SiHa人源宫颈细胞癌中抑制乳酸吸收,IC50为10 nM。
7ACC2 (compound 19; 72 hours) inhibits SiHa cells proliferation in lactate-containing medium with an EC50 of 0.22 μM. In SiHa cells, lactate uptake primarily depends on the high affinity MCT1 transporter.
7ACC2 (compound 19) shows an excellent chemical stability in simulated gastric (SGF) and intestinal (SIF) fluids, a good apparent permeability coefficient (Papp) through Caco-2 monolayer and a high metabolic stability on mouse (MLM) and human liver microsomes (HLM) as well as on human hepatocytes.
7ACC2 is a potent inhibitor of mitochondrial pyruvate transport which consecutively blocks extracellular lactate uptake by promoting intracellular pyruvate accumulation.
7ACC2 (3 mg/kg; intraperitoneal administration; daily; for 5 days or 10days) treatment significantly inhibits tumor growth in mice. 7ACC2 radiosensitizes tumor cells by reducing hypoxia in vivo.
The intraperitoneal administration of 7ACC2 (compound 19; 3 mg/kg) to mice leads to a C
max
of 1246 ng/ml (4 μM) in a very short time (T
max
=10 min) associated with a plasma half-life of 4.5 h.
Animal Model:
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7-week-old female NMRI nude mice with radiotherapy administered
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Dosage:
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3 mg/kg
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Administration:
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Intraperitoneal administration; daily; for 5 days or 10days
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Result:
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A significant increase in tumor growth delay was observed.
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7ACC-2
上下游产品信息
上游原料
下游产品
1472624-85-3, 7ACC-2 相关搜索:
- Inhibitors
- 合成有机化合物配体
- 医药
- 细胞生物学试剂
- 小分子抑制剂
- 小分子抑制剂,天然产物
- MCT抑制剂(7ACC2)
- 7-[苄基(甲基)氨基]-2-氧代-2H-苯并吡喃-3-羧酸
- 1472624-85-3
- 7ACC2,MPC,MCT1,7ACC-2,Monocarboxylate Transporter,Inhibitor,lactate,pyruvate,Mitochondrial Metabolism,radiosensitizes,antitumor,mitochondrial,inhibit
- 2H-1-Benzopyran-3-carboxylic acid, 7-[methyl(phenylmethyl)amino]-2-oxo-
- 7-[benzyl(methyl)amino]-2-oxochromene-3-carboxylic acid
- 7ACC 2; 7ACC-2; 7ACC 2; 7ACC-2
- 7-[Benzyl(methyl)amino]-2-oxo-2H-chromene-3-carboxylic acid
- 7ACC-2
- 7ACC2
- 7ACC 2