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7ACC2
MCT抑制剂 ,7ACC2是MCT高效抑制剂,对[14C]-乳酸流入抑制的IC50值为11nM,是针对癌细胞乳酸转运的新型抗肿瘤分子。
目录号: PC11965 纯度: ≥98%
CAS No. :1472624-85-3
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中文名称
7ACC2
中文别名
7-[苄基(甲基)氨基]-2-氧代-2H-苯并吡喃-3-羧酸
英文名称
7ACC2
英文别名
7ACC-2;7ACC2;compound 19 [PMID: 24095010];7-ACC2;7-(Benzyl(methyl)amino)-2-oxo-2H-chromene-3-carboxylic acid;7-[benzyl(methyl)amino]-2-oxochromene-3-carboxylic acid;7ACC 2;GTPL8818;XTKDQPFUOFAMRL-UHFFFAOYSA-N;BCP11646;BDBM50442711;s6732;AK547419;Q27076338;2-Oxo-7-(methylbenzylamino)-2H-1-benzopyran-3-carboxylic acid;7-[methyl(phenylmethyl)amino]-2-oxo-2H-1-benzopyran-3-carboxylic acid
Cas No.
1472624-85-3
分子式
C18H15NO4
分子量
309.32
包装储存

Sealed and stored at 4℃

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

生物活性

7ACC2 is a potent monocarboxylate transporter (MCT) inhibitor with an IC50 of 11 nM for inhibition of [C]-lactate influx. 7ACC2 is also a potent inhibitor of mitochondrial pyruvate transport. 7ACC2 is an anticancer agent through inhibition of lactate flux.

性状

Solid

IC50 & Target[1][2]

IC50: 11 nM (Monocarboxylate transporter)
Mitochondrial pyruvate transport

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.
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.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

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.
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.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

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

Room temperature or refrigerated transportation.

储存方式

Sealed and stored at 4℃

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

溶解度数据
体外研究: 

DMSO : 50 mg/mL (161.64 mM; Need ultrasonic)

配制储备溶液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
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
*

产品不同,其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液;配成溶液后,建议分装保存,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°C, 6 months; -20°C, 1 month (protect from light)。-80°C 储存时,建议在 6 个月内使用,-20°C 储存时,建议在 1 个月内使用。

体内研究:

建议根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都建议先按照 体外研究 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.

    建议依照次序添加每种溶剂: 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。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH?O 中,得到澄清透明的生理盐水溶液
*
搜索质检报告(COA)

1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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