1472624-85-3|7ACC2|CsnPharm

CAS No.: 1472624-85-3

7ACC2 Catalog No. CSN17889

Synonyms: 7ACC2

7ACC2 is a potent MCT inhibitor with IC50 of 11 nM for inhibition of [14C]-lactate influx for antitumor treatment targeting lactate transport in cancer cells.

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400-920-2911

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实验方案

技术信息

生物活性

描述MCTs (monocarboxylate transporters) are the main carriers of lactate, which was released at a high rate in cancer cells consuming glucose under hypoxia. 7ACC2 is a 7-substituted carboxycoumarins and quinolinone derivative which can inhibit lactate flux in SiHa cells with IC50 value of 11nM. 7ACC2 was previously regarded as an MCT inhibitor. However, recently it was found that 7ACC2 did not inhibits MCT1 activity in MCT1-expressing Xenopus oocytes. The inhibition of lactate flux by 7ACC2 may be MCT1- and MCT4-independent. Treatment with 10μM 7ACC2 for 24h stimulated lactate release of SiHa cells cultured in glucose-containing medium and led to extracellular acidification. Pyruvate metabolism may be another target of 7ACC2 and the inhibition of mitochondrial pyruvate transport consecutively blocked extracellular lactate uptake by promoting intracellular pyruvate accumulation. Also this would induce cytotoxic effects together with glycolysis stimulation and uncompensated inhibition of mitochondrial respiration. The inhibition of mitochondrial pyruvate transport by daily intraperitoneal injection with 3 mg/kg 7ACC2 for 10 or 5 days could radiosensitize tumor cells by reducing hypoxia in SiHa xenograft nude mice.
动物研究
剂量
Nude Mice: 3 mg/kg^[2] (i.p.)

给药途径
i.p.
参考文献

动物研究
剂量	Nude Mice: 3 mg/kg^[2] (i.p.)
给药途径	i.p.

[1] Draoui N, Schicke O, et al. Synthesis and pharmacological evaluation of carboxycoumarins as a new antitumor treatment targeting lactate transport in cancer cells. Bioorg Med Chem. 2013 Nov 15;21(22):7107-17.
[2] Corbet C, Bastien E, et al. Interruption of lactate uptake by inhibiting mitochondrial pyruvate transport unravels direct antitumor and radiosensitizing effects. Nat Commun. 2018 Mar 23;9(1):1208.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 3.2329 mL
- 16.1647 mL
- 32.3294 mL
- 5 mM
- 0.6466 mL
- 3.2329 mL
- 6.4659 mL
- 10 mM
- 0.3233 mL
- 1.6165 mL
- 3.2329 mL

技术信息

CAS号

1472624-85-3

储存条件

粉末: Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C18H15NO4

运输

蓝冰

分子量

309.32

别名

7ACC2

溶解度

DMSO	62.0 mg/mL (200.4 mM)
Water	insoluble

动物实验配方

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