7ACC2

7ACC2 is a potent monocarboxylate transporter (MCT) inhibitor with an IC₅₀ of 11 nM for inhibition of [¹⁴C]-lactate influx. 7ACC2 is also a potent inhibitor of mitochondrial pyruvate transport. 7ACC2 is an anticancer agent through inhibition of lactate flux^[1][2]. IC50 & Target: IC50: 11 nM (Monocarboxylate transporter)^[1]
Mitochondrial pyruvate transport^[2] In Vitro: 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^[1].
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^[1].
7ACC2 is a potent inhibitor of mitochondrial pyruvate transport which consecutively blocks extracellular lactate uptake by promoting intracellular pyruvate accumulation^[2]. In Vivo: 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^[2].
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^[1].