7ACC2

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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。

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 C_maxof 1246 ng/ml (4 μM) in a very short time (T_max=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 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

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。