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7ACC2
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
7ACC2图片
CAS NO:1472624-85-3
包装与价格:
包装价格(元)
10 mM * 1 mL in DMSO电议
2mg电议
5mg电议
10mg电议
50mg电议
100mg电议

产品介绍
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].

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.
分子量

309.32

性状

Solid

Formula

C18H15NO4

CAS 号

1472624-85-3

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
浓度溶剂体积质量1 mg5 mg10 mg
1 mM3.2329 mL16.1645 mL32.3290 mL
5 mM0.6466 mL3.2329 mL6.4658 mL
10 mM0.3233 mL1.6164 mL3.2329 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。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH2O 中,得到澄清透明的生理盐水溶液
*以上所有助溶剂都可在本网站选购。