Ethacrynic Acid

Ethacrynic acid is a loop diuretic with anticancer activity., It inhibits the Na-K-2Cl (NKCC) cotransporter in duck erythrocytes (IC50 = 0.18 mM) and ATP-dependent chloride uptake in rat renal plasma membrane vesicles when used at a concentration of 0.3 mM., Ethacrynic acid also inhibits glutathione S-transferase P1-1 (GSTP1-1) and GSTA3-3 (IC50s = 4.9 and ~0.4 µM, respectively), and inhibits Wnt/beta-catenin signaling in a cell-based reporter assay. It is cytotoxic to primary chronic lymphocytic leukemia cells (IC50 = 8.56 µM), as well as MCF-7, MDA-MB-231, and 4T1 cancer cells (IC50s = 45.53, 39.64, and 25.23 µM, respectively). Ethacrynic acid (250 µg per day) increases tumor growth reduction induced by the EGFR family inhibitors afatinib (Cay-11492, Cay-21567) or neratinib (Cay-18404) in a 4T1 murine breast cancer model. Formulations containing ethacrynic acid have been used in the treatment of edema.Formal Name: 2-[2,3-dichloro-4-(2-methylene-1-oxobutyl)phenoxy]-acetic acid. CAS Number: 58-54-8. Synonyms: MK-595, NSC 85791, NSC 624008. Molecular Formula: C13H12Cl2O4. Formula Weight: 303.1. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 30 mg/ml, DMSO: 30 mg/ml, Ethanol: 30 mg/ml, Ethanol:PBS (pH 7.2) (1:1): 0.5 mg/ml. lambdamax: 270 nm. SMILES: O=C(C(CC)=C)C1=C(Cl)C(Cl)=C(OCC(O)=O)C=C1. InChi Code: InChI=1S/C13H12Cl2O4/c1-3-7(2)13(18)8-4-5-9(12(15)11(8)14)19-6-10(16)17/h4-5H,2-3,6H2,1H3,(H,16,17). InChi Key: AVOLMBLBETYQHX-UHFFFAOYSA-N.