Description
Product Information
| Molecular Weight: | 555.55 |
| Formula: | C27H28F3N7O3 |
| Purity: | >98% |
| CAS#: | 1374640-70-6 |
| Solubility: | DMSO: ≥ 43 mg/mL |
| Chemical Name: | N-(3-((2-((4-(4-acetylpiperazin-1-yl)-2-methoxyphenyl)amino)-5-(trifluoromethyl)pyrimidin-4-yl)amino)phenyl)acrylamide |
| Storage: | Powder -20oC 3 years 4oC 2 years In solvent -80oC 6 months -20oC 1 month |
Biological Activity:
CO-1686 is an orally delivered kinase inhibitor that specifically targets the mutant forms of EGFR including T790M, and the Ki values for EGFRL858R/T790M and EGFRWT are 21.5 nM and 303.3 nM, respectively.
How to use:
In Vitro: CO-1686 (0.1 μM) inhibits EGFR potently and irreversibly, and inhibits more than 50% of 23 targets. CO-1686 potently and selectively inhibits growth of NSCLC cells expressing mutant EGFR and induces apoptosis. CO-1686 resistant NSCLC cell lines are sensitive to AKT inhibition[1].
In Vivo: CO-1686 (100 mg/kg/day, p.o.) demonstrates anti-tumor activity in NSCLC EGFR mutant xenograft models. CO-1686 (50 mg/kg bid, p.o.) demonstrates anti-tumor activity in human EGFR-L858R and EGFR-L858R-T790M expressing transgenic mice[1].
Reference:
[1]. Walter AO, et al. Discovery of a mutant-selective covalent inhibitor of EGFR that overcomes T790M-mediated resistance in NSCLC. Cancer Discov. 2013 Sep 25.
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