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7ACC1的可视化放大

7ACC1

A fluorescent probe

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7ACC1的二维码
  • 库存: 现货
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  • 货号: ajci11624
  • CAS: 50995-74-9
  • 别名: 香豆素D1421; DEAC; Coumarin D 1421; D 1421
  • 分子式: C14H15NO4
  • 分子量: 261.27
  • 纯度: >98%
  • 溶解度: ≥ 13.05mg/mL in DMSO
  • 储存: 4°C, protect from light
  • 库存: 现货

Background

7ACC1(DEAC; Coumarin D 1421; D 1421) selectively interfere with lactate fluxes in the lactate-rich tumor microenvironment; inhibits lactate influx but not efflux in tumor cells expressing MCT1 and MCT4 transporters.IC50 value: 0.86 uM(Lactate uptake inhibition) [1]Target: MCT inhibitor; lactate transport inhibitorContrary to the reference MCT1 inhibitor AR-C155858, 7ACC unexpectedly inhibited lactate influx but not efflux in tumor cells expressing MCT1 and MCT4 transporters. 7ACC delayed the growth of cervix SiHa tumors, colorectal HCT116 tumors, and orthoptopic MCF-7 breast tumors. MCT target engagement was confirmed by the lack of activity of 7ACC on bladder UM-UC-3 carcinoma that does not express functional MCT. 7ACC also inhibited SiHa tumor relapse after treatment with cisplatin. Finally, we found that contrary to AR-C155858, 7ACC did not prevent the cell entry of the substrate-mimetic drug 3-bromopyruvate (3BP) through MCT1, and contributed to the inhibition of tumor relapse after 3BP treatment.


参考文献:
[1]. Draoui N, 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.

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