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7ACC1 Sale

(Synonyms: 香豆素D1421; DEAC; Coumarin D 1421; D 1421) 目录号 : GC13691

A fluorescent probe

7ACC1 Chemical Structure

Cas No.:50995-74-9

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Sample solution is provided at 25 µL, 10mM.

Description

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.

化学性质

Cas No. 50995-74-9 SDF
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
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1 mg 5 mg 10 mg
1 mM 3.8275 mL 19.1373 mL 38.2746 mL
5 mM 0.7655 mL 3.8275 mL 7.6549 mL
10 mM 0.3827 mL 1.9137 mL 3.8275 mL
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