
CNX-2006
CAS No. 1375465-09-0
CNX-2006( CNX2006 | CNX 2006 | CNX-2006. )
Catalog No. M17265 CAS No. 1375465-09-0
CNX-2006 is a novel irreversible mutant-selective EGFR inhibitor with IC50 of < 20 nM, with very weak inhibition at wild-type EGFR.
Purity : >98% (HPLC)






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Biological Information
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Product NameCNX-2006
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NoteResearch use only, not for human use.
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Brief DescriptionCNX-2006 is a novel irreversible mutant-selective EGFR inhibitor with IC50 of < 20 nM, with very weak inhibition at wild-type EGFR.
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DescriptionCNX-2006 is a potent, mutant-selective EGFR inhibitor with excellent in vitro activity in cells with activating EGFR mutations, as well as in cells harbouring the T790M mutation. CNX-2006 is the prototype for CO-1686, which is currently in a Phase I clinical trial for the treatment of EGFR-mutant lung cancer.
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In VitroCNX-2006 inhibits EGFR-T790M cells growth up to 1000-fold more compared to wild-type EGFR cells. EGFR inhibition is observed in cells harbouring the T790M mutation at IC50 values below 20 nM after 1 hour exposure to the drug. CNX-2006 also significantly reduces the volume of tumor spheres derived from H1975 cells. CNX-2006 exhibits specificity and potent activity against T790M. The drug also shows activity against uncommon EGFR mutations including G719S, L861Q, an exon 19 insertion mutant (I744-K745insKIPVAI), and T854A, but not an exon 20 insertion (H773-V774HVdup). In an in vitro resistance model, CNX-2006 significantly inhibits the emergence of resistant cells. Chronic exposure to escalating doses of CNX-2006 fails to select for and/or enhance T790M-mediated resistance using PC-9 or HCC827 cells (both harboring exon 19 deletions), or PC-9/ER and HCC827/ER cells with existing T790M and resistance to erlotinib.
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In Vivo——
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SynonymsCNX2006 | CNX 2006 | CNX-2006.
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PathwayPI3K/Akt/mTOR signaling
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TargetmTOR
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RecptorEGFR (mutant)
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Research AreaCancer
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Indication——
Chemical Information
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CAS Number1375465-09-0
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Formula Weight545.53
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Molecular FormulaC26H27F4N7O2
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Purity>98% (HPLC)
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SolubilityDMSO : ≥ 52 mg/mL. 95.32 mM
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SMILESCOc1c(Nc2ncc(c(Nc3cccc(NC(=O)C=C)c3)n2)C(F)(F)F)ccc(NC2CN(CCF)C2)c1
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Chemical NameN-(3-((2-((4-((1-(2-fluoroethyl)azetidin-3-yl)amino)-2-methoxyphenyl)amino)-5-(trifluoromethyl)pyrimidin-4-yl)amino)phenyl)acrylamide
Shipping & Storage Information
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Storage(-20℃)
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ShippingWith Ice Pack
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Stability≥ 2 years
Reference
1. Ohashi K, et al. 2013
molnova catalog



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