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Chemical Structure : CNX2006
CAS No.: 1375465-09-0
Catalog No.: PC-38035Not For Human Use, Lab Use Only.
CNX2006 (CNX-2006) is a potent, covalent, mutant-selective EGFR inhibitor with IC50 of <20 nM, weak inhibition at wild-type EGFR.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 25 mg | $258 | In stock | |
| 50 mg | $458 | In stock | |
| 100 mg | $758 | In stock | |
| 500 mg | Get quote |
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CNX2006 (CNX-2006) is a potent, covalent, mutant-selective EGFR inhibitor with IC50 of <20 nM, weak inhibition at wild-type EGFR.
CNX2006 inhibits the phosphorylation of EGFR-T790M alone or the T790M mutation in cis with activating mutations with IC50 of 46 and 61 nM in NSCLC cell lines NCI-H1975 and PC9GR4, respectively.
CNX-2006 affected the WT-EGFR only at concentrations 10-fold higher than the ones necessary to inhibit mutated receptor.
CNX-2006 is also active against rare EGFR mutations, including EGFR-G719S, -ex19ins (I744-K745insKIPVAI), -L861Q, -ex20ins (H773-V774HVdup), and -T854A.
CNX-2006 inhibits mutant-EGFR cell proliferation by inducing apoptosis in vitro. CNX-2006 inhibits EGFR-T790M tumor growth in vivo.
| M.Wt | 545.53 | |
| Formula | C26H27F4N7O2 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| Chemical Name/SMILES |
N-(3-((2-((4-((1-(2-fluoroethyl)azetidin-3-yl)amino)-2-methoxyphenyl)amino)-5-(trifluoromethyl)pyrimidin-4-yl)amino)phenyl)acrylamide |
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1. Galvani E, et al. Oncotarget. 2015 Dec 15;6(40):42717-32.
2. Mizuuchi H, et al. Cancer Sci. 2016 Apr;107(4):461-8.
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