中文名 | 7ACC2 |
英文名 | 7ACC2 |
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 |
英文别名 | 7ACC2 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- |
CAS | 1472624-85-3 |
EINECS | 604-604-1 |
化学式 | C18H15NO4 |
分子量 | 309.32 |
密度 | 1.368±0.06 g/cm3(Predicted) |
沸点 | 548.9±50.0 °C(Predicted) |
溶解度 | DMSO: ≥ 46 mg/mL |
酸度系数 | -98.37±0.20(Predicted) |
存储条件 | 2-8°C |
体外研究 | 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. |
体内研究 | 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: 7-week-old female NMRI nude mice with radiotherapy administered Dosage: 3 mg/kg Administration: Intraperitoneal administration; daily; for 5 days or 10days Result: A significant increase in tumor growth delay was observed. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 3.233 ml | 16.165 ml | 32.329 ml |
5 mM | 0.647 ml | 3.233 ml | 6.466 ml |
10 mM | 0.323 ml | 1.616 ml | 3.233 ml |
5 mM | 0.065 ml | 0.323 ml | 0.647 ml |
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