CNX-2006

• CAT Number: I001449
• CAS Number: 1375465-09-0
• Molecular Formula: C26H27F4N7O2
• Molecular Weight: 545.53
• Purity: ≥95%
• Target: Mutant EGFR
• Solubility: DMSO: ≥ 52 mg/mL
• Storage: Store at -20°C
• IC50: <20 nM
• IUPAC Name: N-[3-[[2-[4-[[1-(2-fluoroethyl)azetidin-3-yl]amino]-2-methoxyanilino]-5-(trifluoromethyl)pyrimidin-4-yl]amino]phenyl]prop-2-enamide
• InChI: InChI=1S/C26H27F4N7O2/c1-3-23(38)33-16-5-4-6-17(11-16)34-24-20(26(28,29)30)13-31-25(36-24)35-21-8-7-18(12-22(21)39-2)32-19-14-37(15-19)10-9-27/h3-8,11-13,19,32H,1,9-10,14-15H2,2H3,(H,33,38)(H2,31,34,35,36)
• InChIKey: BFSRTTWIPACGMI-UHFFFAOYSA-N
• SMILES: COC1=C(C=CC(=C1)NC2CN(C2)CCF)NC3=NC=C(C(=N3)NC4=CC(=CC=C4)NC(=O)C=C)C(F)(F)F

CNX-2006 (Cat.No:I001449) is a novel, irreversible, mutation-selective EGFR inhibitor with an IC50 of <20nM, exhibiting weak inhibition against wild-type EGFR. In vitro studies demonstrate that CNX-2006 is a potent inhibitor of EGFR mutations, especially the T790M mutation, with slower development of resistance compared to erlotinib. In vivo studies show effectiveness of CNX-2006 in H1975 (EGFRL858R/T790M) tumor models.

Reference

[1]. Kadoaki Ohashi, et al. CNX-2006, a Novel Irreversible Epidermal Growth Factor Receptor (EGFR) Inhibitor, Selectively Inhibits EGFR T790M and Fails to Induce T790M-Mediated Resistance In Vitro
[2]. Elena Galvani, et al. Role of epithelial-mesenchymal transition (EMT) in sensitivity to CNX- 2006,a novel mutant-selective EGFR inhibitor which overcomes in vitro T790M-mediated resistance in NSCLC