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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.
| 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 |
| Solubility | DMSO 100 mg/mL (180.0 mM) Water Insoluble Ethanol Insoluble |
| Appearance | Off-white powder |
| Store Temp | 4°C |
|---|---|
| Ship Temp | Ambient |
| MSDS | |
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| Info Sheet |
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.