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.