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AG-1478

AG-1478 is an inhibitor of EGFR that exhibits anticancer, anti-inflammatory, and anti-asthma activities. AG-1478 inhibits proliferation of hepatocellular carcinoma cells but potential use is limited by poor solubility. In bronchial epithelial cells, this compound decreases goblet cell number and mucus hypersecretion. AG-1478 also suppresses secretion of MUC5AC, VEGF, and IL-8 in airway epithelial cells, potentially preventing airway inflammation and remodeling.

References PubMed ID::http://www.ncbi.nlm.nih.gov/pubmed/18837291

Cas No.

153436-53-4

Formula

C16H14ClN3O2

Formula Wt.

315.76

IUPAC Name

n-(3-chlorphenyl)-6,7-dimethoxy-4-chinazolinamin

Synonym

Tyrphostin AG1478, NSC693255

Parker JC, Douglas I, Bell J, et al. Epidermal Growth Factor Removal or Tyrphostin AG1478 Treatment Reduces Goblet Cells & Mucus Secretion of Epithelial Cells from Asthmatic Children Using the Air-Liquid Interface Model. PLoS One. 2015 Jun 9;10(6):e0129546. PMID: 26057128.

Bondì ML, Azzolina A, Craparo EF, et al. Entrapment of an EGFR inhibitor into nanostructured lipid carriers (NLC) improves its antitumor activity against human hepatocarcinoma cells. J Nanobiotechnology. 2014 May 12;12:21. PMID: 24886097.

Shimizu S, Kouzaki H, Ogawa T, et al. Eosinophil-epithelial cell interactions stimulate the production of MUC5AC mucin and profibrotic cytokines involved in airway tissue remodeling. Am J Rhinol Allergy. 2014 Mar-Apr;28(2):103-9. PMID: 24717945.

PLX-4720