50995-74-9

50995-74-9 structure

Name: 7-Diethylaminocoumarin-3-carboxylic acid
Chemical Name: 7-(Diethylamino)coumarin-3-carboxylic acid
CAS Number: 50995-74-9
Molecular Formula: C₁₄H₁₅NO₄
Molecular Weight: 261.273
Catalog: Signaling Pathways Membrane Transporter/Ion Channel Monocarboxylate Transporter
Create Date: 2018-12-01 18:52:47
Modify Date: 2024-01-02 19:26:07
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.

Name	7-(Diethylamino)coumarin-3-carboxylic acid
Synonyms	7-diethylaminocoumarin-3-carboxylic acid 7-(Diethylamino)coumarin-3-carboxylic Acid 2H-1-Benzopyran-3-carboxylic acid, 7-(diethylamino)-2-oxo- 7-(Diethylamino)-2-oxo-2H-chromene-3-carboxylic acid 7-(diethylamino)-2-oxochromene-3-carboxylic acid 7ACC1

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.
Related Catalog	Signaling Pathways >> Membrane Transporter/Ion Channel >> Monocarboxylate Transporter Research Areas >> Cancer
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.

Personal Protective Equipment	Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter
Hazard Codes	Xi
Safety Phrases	22-24/25
RIDADR	NONH for all modes of transport
HS Code	2932209090

HS Code	2932209090
Summary	2932209090. other lactones. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%