7ACC1（DEAC；香豆素 D 1421；D 1421）选择性地干扰富含乳酸的肿瘤微环境中的乳酸通量；抑制表达 MCT1 和 MCT4 转运蛋白的肿瘤细胞中的乳酸流入，但不抑制流出。
| Cas No. | 50995-74-9 |
| 别名 | 香豆素D1421; DEAC; Coumarin D 1421; D 1421 |
| 化学名 | 7-(diethylamino)-2-oxochromene-3-carboxylic acid |
| Canonical SMILES | CCN(CC)C1=CC2=C(C=C1)C=C(C(=O)O2)C(=O)O |
| 分子式 | C14H15NO4 |
| 分子量 | 261.27 |
| 溶解度 | ≥ 13.05mg/mL in DMSO |
| 储存条件 | 4°C, protect from light |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request |
| 产品描述 | 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. References:
[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. |
