| 產(chǎn)品描述： | 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 |
| 靶點(diǎn)： |
IC50: 11 nM (Monocarboxylate transporter) Mitochondrial pyruvate transport;MitochondrialMetabolism;?Monocarboxylatetransporter |
| 體外研究： |
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 |
| 體內(nèi)研究： |
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[2] Dosage: 3?mg/kg Administration: Intraperitoneal administration; daily; for 5 days or 10days Result: A significant increase in tumor growth delay was observed. |
| 溶解性： |
Soluble in DMSO |
| 保存條件： |
-20℃ |
| 配置溶液濃度參考： |
|
1mg |
5mg |
10mg |
| 1 mM |
3.233 ml |
16.165 ml |
32.329 ml |
| 5 mM |
0.647 ml |
3.233 ml |
6.466 ml |
| 10 mM |
0.323 ml |
1.616 ml |
3.233 ml |
| 50 mM |
0.065 ml |
0.323 ml |
0.647 ml |
|
| 注意： |
部分產(chǎn)品我司僅能提供部分信息，我司不保證所提供信息的權(quán)威性，僅供客戶參考交流研究之用。 |
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