中文同义词:
7-[苄基(甲基)氨基]-2-氧代-2H-苯并吡喃-3-羧酸;MCT抑制剂(7ACC2)
英文同义词:
7ACC 2;7ACC2;7ACC-2;7-[Benzyl(methyl)amino]-2-oxo-2H-chromene-3-carboxylic acid;7ACC 2; 7ACC-2; 7ACC 2; 7ACC-2;7-[benzyl(methyl)amino]-2-oxochromene-3-carboxylic acid;2H-1-Benzopyran-3-carboxylic acid, 7-[methyl(phenylmethyl)amino]-2-oxo-
相关类别:
细胞生物学试剂;小分子抑制剂，天然产物;小分子抑制剂;医药;Inhibitors
沸点
548.9±50.0 °C(Predicted)
密度
1.368±0.06 g/cm3(Predicted)
酸度系数(pKa)
-98.37±0.20(Predicted)
生物活性
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。
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.
Animal Model:
7-week-old female NMRI nude mice with radiotherapy administered
Administration:
Intraperitoneal administration; daily; for 5 days or 10days
Result:
A significant increase in tumor growth delay was observed.
