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CO-1686

CO-1686 is an inhibitor of mutant forms of EGFR, including T790M EGFR. CO-1686 exhibits anticancer chemotherapeutic activity, inducing tumor regression in animal models of non-small cell lung cancer (NSCLC) and sensitizing cancer cells in vitro to other chemotherapeutics.

References PubMed ID::http://www.ncbi.nlm.nih.gov/pubmed/18852894

Cas No.

1374640-70-6

Purity

≥98%

Formula

C27H28F3N7O3

Formula Wt.

555.55

Chemical Name

N-(3-((2-((4-(4-Acetylpiperazin-1-yl)-2-methoxyphenyl)amino)-5-(trifluoromethyl)pyrimidin-4-yl)amino)phenyl)prop-2-enamide

IUPAC Name

N-[3-[[2-[4-(4-acetylpiperazin-1-yl)-2-methoxyanilino]-5-(trifluoromethyl)pyrimidin-4-yl]amino]phenyl]prop-2-enamide

Synonym

AVL-301; Rociletinib

Appearance

Off-white powder

Walter AO, Sjin RT, Haringsma HJ, et al. Discovery of a mutant-selective covalent inhibitor of EGFR that overcomes T790M-mediated resistance in NSCLC. Cancer Discov. 2013 Dec;3(12):1404-15. PMID: 24065731.

Yu HA, Riely GJ. Second-generation epidermal growth factor receptor tyrosine kinase inhibitors in lung cancers. J Natl Compr Canc Netw. 2013 Feb 1;11(2):161-9. PMID: 23411383.

ABBV-075