7ACC2 是一种有效的单羧酸盐转运蛋白 (MCT) 抑制剂,IC50为 11 nM,可抑制乳酸涌入。7ACC2 还是一种线粒体丙酮酸转运 (mitochondrial pyruvate transport) 的有效抑制剂。7ACC2 通过抑制乳酸通量来发挥抗癌作用。
生物活性 | 7ACC2 is a potentmonocarboxylate transporter(MCT)inhibitor with anIC50of 11 nM for inhibition of [14C]-lactate influx. 7ACC2 is also a potent inhibitor ofmitochondrial 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] |
体外研究 (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].
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体内研究 (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 Cmaxof 1246 ng/ml (4 μM) in a very short time (Tmax=10 min) associated with a plasma half-life of 4.5 h[1].
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. |
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运输条件 | Room temperature in continental US; may vary elsewhere. |
储存方式 | 4°C, protect from light *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light) |
溶解性数据 | In Vitro: DMSO : 50 mg/mL(161.64 mM;Need ultrasonic) 配制储备液 1 mM | 3.2329 mL | 16.1645 mL | 32.3290 mL | 5 mM | 0.6466 mL | 3.2329 mL | 6.4658 mL | 10 mM | 0.3233 mL | 1.6164 mL | 3.2329 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 储备液的保存方式和期限:-80℃, 6 months; -20℃, 1 month (protect from light)。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用;
以下溶剂前显示的百 分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂: 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: 2.5 mg/mL (8.08 mM); Suspended solution; Need ultrasonic
此方案可获得 2.5 mg/mL (8.08 mM) 的均匀悬浊液,悬浊液可用于口服和腹腔注射。 以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。 *以上所有助溶剂都可在本网站选购。
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