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)

COA Datasheet HNMR HPLC MSDS Handing Instructions
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5MG 68 In Stock
10MG 115 In Stock
25MG 212 In Stock
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Biological Information

  • Product Name
    CNX-2006
  • Note
    Research use only, not for human use.
  • Brief Description
    CNX-2006 is a novel irreversible mutant-selective EGFR inhibitor with IC50 of < 20 nM, with very weak inhibition at wild-type EGFR.
  • Description
    CNX-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.
  • In Vitro
    CNX-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.
  • In Vivo
    ——
  • Synonyms
    CNX2006 | CNX 2006 | CNX-2006.
  • Pathway
    PI3K/Akt/mTOR signaling
  • Target
    mTOR
  • Recptor
    EGFR (mutant)
  • Research Area
    Cancer
  • Indication
    ——

Chemical Information

  • CAS Number
    1375465-09-0
  • Formula Weight
    545.53
  • Molecular Formula
    C26H27F4N7O2
  • Purity
    >98% (HPLC)
  • Solubility
    DMSO : ≥ 52 mg/mL. 95.32 mM
  • SMILES
    COc1c(Nc2ncc(c(Nc3cccc(NC(=O)C=C)c3)n2)C(F)(F)F)ccc(NC2CN(CCF)C2)c1
  • Chemical Name
    N-(3-((2-((4-((1-(2-fluoroethyl)azetidin-3-yl)amino)-2-methoxyphenyl)amino)-5-(trifluoromethyl)pyrimidin-4-yl)amino)phenyl)acrylamide

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

1. Ohashi K, et al. 2013
molnova catalog
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