|7-(二乙氨基)-2-氧代-2H-苯并吡喃-3-羧酸|CsnPharm

CAS No.: 50995-74-9

香豆素D1421 Catalog No. CSN12098

Synonyms: 香豆素D1421;DEAC;Coumarin D 1421

7ACC1 selectively interfere with lactate fluxes in the lactate-rich tumor microenvironment and inhibits lactate influx but not efflux in tumor cells expressing MCT1 and MCT4 transporters.

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400-920-2911

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生物活性

实验方案

技术信息

生物活性

描述7ACC1 is a 7-aminocarboxycoumarins (7ACC) derivative which can inhibit lactate flux but not lactate efflux in the lactate-rich tumor microenvironment. Treatment with 10μM 7ACC1 inhibited lactate influx but not lactate efflux in SiHa cells, FaDu cells and Hela cells at 24h and inhibited proliferation of SiHa cells at 72h, but not HL60, MDA-MD-231, hTERT BJ-5ta, HUVECs or embryonic kidney cells. Inhibition of MCT4 by 100μM 7ACC1 could enhance the cytotoxicity of NK cells through elevating pH value and decreasing extracellular lactate flow content of coculture cell supernatants. This may reverse the acidified tumor microenvironment and contribute to the inhibitory effect of breast cancer growth in Balb/c mice inoculated with 4T1 cells pretreated with 100μM 7ACC1. Similar effect of 7ACC1 in vivo could be observed as daily administration of 3 mg/kg 7ACC1 intraperitoneally for 12 or 21 days could inhibit tumor growth of mice xenograft SiHa, HCT116 and MCF-7 tumors.
动物研究
剂量
Mice: 0.003 mg/kg - 0.3 mg/kg^[2] (i.p.) Rat: 150 mg/kg - 300 mg/kg^[3] (i.p.)

给药途径
i.p.
参考文献

动物研究
剂量	Mice: 0.003 mg/kg - 0.3 mg/kg^[2] (i.p.) Rat: 150 mg/kg - 300 mg/kg^[3] (i.p.)
给药途径	i.p.

[1] Draoui N, Schicke O, et al. Antitumor activity of 7-aminocarboxycoumarin derivatives, a new class of potent inhibitors of lactate influx but not efflux. Mol Cancer Ther. 2014 Jun;13(6):1410-8.
[2] Long Y, Gao Z, et al. Downregulation of MCT4 for lactate exchange promotes the cytotoxicity of NK cells in breast carcinoma. Cancer Med. 2018 Sep;7(9):4690-4700.

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
- 3.8274 mL
- 19.1371 mL
- 38.2741 mL
- 5 mM
- 0.7655 mL
- 3.8274 mL
- 7.6548 mL
- 10 mM
- 0.3827 mL
- 1.9137 mL
- 3.8274 mL

技术信息

CAS号

50995-74-9

储存条件

粉末: Keep in dark place,Inert atmosphere,Room temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C14H15NO4

运输

蓝冰

分子量

261.27

别名

香豆素D1421;DEAC;Coumarin D 1421;D 1421

溶解度

DMSO	30.0 mg/mL (114.8 mM) warming

动物实验配方

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