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MedChemExpress - Model 7ACC2 -1472624-85-3
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].MCE products for research use only. We do not sell to patients.
7ACC2
MCE China：7ACC2
Brand：MedChemExpress (MCE)
Cat. No.HY-D0713
CAS：1472624-85-3
Purity：99.62%
Storage：4°C, protect from light *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Shipping：Room temperature in continental US; may vary elsewhere.
Description：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.
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 Cmax of 1246 ng/ml (4 μM) in a very short time (Tmax=10 min) associated with a plasma half-life of 4.5 h[1].
IC50 & Target：IC50: 11 nM (Monocarboxylate transporter)[1] Mitochondrial pyruvate transport[2] Cellular Effect Cell Line Type Value Description References
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References：
[1]. Draoui N, et al. Synthesis and pharmacological evaluation of carboxycoumarins as a new antitumor treatment targeting lactate transport in cancer cells. Bioorg Med Chem. 2013 Nov 15;21(22):7107-17. [Content Brief]
[2]. Cyril Corbet, et al. Interruption of lactate uptake by inhibiting mitochondrial pyruvate transport unravels direct antitumor and radiosensitizing effects. Nat Commun. 2018 Mar 23;9(1):1208. [Content Brief]
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