7ACC2

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

7ACC2 是一种新型强效 MCT 抑制剂，抑制 [14C]-乳酸流入，IC50 为 11 nM；针对 Y 细胞中乳酸转运的新抗肿瘤治疗。

7ACC2 is a new potent MCT inhibitor with IC50 of 11 nM for inhibition of [14C]-lactate influx; new antitumor treatment targeting lactate transport in Y cells.

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 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. Animal Model:7-week-old female NMRI nude mice with radiotherapy administered Dosage:3?mg/kg Administration:Intraperitoneal administration; daily; for 5 days or 10daysResult:A significant increase in tumor growth delay was observed.

7ACC2 | 7 ACC2 | 7-ACC2

Membrane Transporter/Ion Channel

Monocarboxylate Transporter

lactate transport

Cancer

——

1472624-85-3

309.32

C18H15NO4

>98% (HPLC)

DMSO: 46 mg/mL

O=C1C(C(O)=O)=CC2=CC=C(N(CC3=CC=CC=C3)C)C=C2O1

7-(benzyl(methyl)amino)-2-oxo-2H-chromene-3-carboxylic acid

(-20℃)

With Ice Pack

≥ 2 years