CNX-2006
CNX-2006, a structural analog of CO-1686, is a selective and irreversible inhibitor of mutant-EGFR with IC50 value of < 20 nM.
The epidermal growth factor receptor (EGFR) is the cell-surface receptor for epidermal growth factor and plays an important role in tumor invasion and cancer cell proliferation.
CNX-2006 is a novel and irreversible mutant-selective EGFR inhibitor with very weak inhibition of wild-type EGFR. In non-small cell lung cancer (NSCLC) models expressing mutant EGFR-T790M, CNX-2006 inhibited EGFR signaling. CNX-2006 acquired resistance which was drove by NF-κB. So NF-κB activation might replace the EGFR signaling. These results suggested that inhibition of NF-κB pathway was a promising therapy method for patients who progressed after treatment with mutant-selective EGFR inhibitors [1].
Reference:
Galvani E, Sun J, Leon LG, et al. NF-κB drives acquired resistance to a novel mutant-selective EGFR inhibitor. Oncotarget, 2015.
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 545.53 |
| Cas No. | 1375465-09-0 |
| Formula | C26H27F4N7O2 |
| Solubility | ≥27.3 mg/mL in DMSO |
| Chemical Name | N-(3-((2-((4-((1-(2-fluoroethyl)azetidin-3-yl)amino)-2-methoxyphenyl)amino)-5-(trifluoromethyl)pyrimidin-4-yl)amino)phenyl)acrylamide |
| SDF | Download SDF |
| Canonical SMILES | FC(F)(F)C1=C(NC2=CC(NC(C=C)=O)=CC=C2)N=C(NC3=CC=C(NC4CN(CCF)C4)C=C3OC)N=C1 |
| Shipping Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
| General tips | We do not recommend long-term storage for the solution, please use it up soon. |
Quality Control & MSDS
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Chemical structure
