biological activity | 7ACC2 is a potent MCT1 inhibitor that inhibits lactate absorption in human-derived cervical cell carcinoma of SiHa, the IC50 was 10 nM. |
Target | TargetValue MCT1 () |
Target | Value |
in vitro study | 7ACC2 (compound 19; 72 hours) inhibit SiHa cells in lactate-containing medium with an EC50 of 0.22 μm. In SiHa cells, lactate uptake primary costs on the high affinity MCT1 transporter. 7ACC2 (compound 19) show an excellent chemical stability in simulated gastric (SGF) and Intel Intal (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. |
in vivo study | 7ACC2 (3 mg/kg; Intraparoneal administration; daily; for 5 days or 10days) refer to significantly inhibits tumor growth in mice. 7ACC2 radiosentizes tumor cells by reducing hypoxia in vivo. The intrapeach 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 |
Dosage:
| 3 mg/kg |
Administration:
| Intraperitoneal administration; daily; for 5 days or 10days |
Result:
| A significant increase in tumor growth delay was observed. |