| 中文名称 | 7ACC-2 |
| 英文名称 | 7ACC-2 |
| CAS号 | 1472624-85-3 |
| 分子式 | C18H15NO4 |
| 分子量 | 309.32 |
| EINECS号 | 604-604-1 |
| 沸点 | 548.9±50.0 °C(Predicted) |
| 密度 | 1.368±0.06 g/cm3(Predicted) |
| 溶解度 | 不溶于乙醇；不溶于水； DMSO 中≥47.5 mg/mL |
| 形态 | 粉末 |
| 酸度系数(pKa) | -98.37±0.20(Predicted) |
| 颜色 | 浅黄至黄色 |
| 海关编码 | 2932990090 |
| Target | Value |
|
MCT1
() |
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: | 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. |