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    CNX-2006
    CNX-2006

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V0548
    CAS #: 1375465-09-0Purity ≥98%

    Description: CNX-2006 (CNX2006), a CO-1686 analog, is a covalent / irreversible and mutant-selective EGFR inhibitor with potential antitumor activity. It inhibits EGFR with an IC50 of < 20 nM. CNX-2006 is structurally similar to CO-1686, which is currently in clinical trials for treating lung cancer.  

    References: Galvani E, Sun J, Leon LG, et al.  Oncotarget, 2015.

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    Molecular Weight (MW)545.53
    FormulaC26H27F4N7O2
    CAS No.1375465-09-0
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 100 mg/mL (183.3 mM)
    Water: <1 mg/mL
    Ethanol: 29 mg/mL (53.1 mM)
    Other info

    Chemical Name: N-(3-((2-((4-((1-(2-fluoroethyl)azetidin-3-yl)amino)-2-methoxyphenyl)amino)-5-(trifluoromethyl)pyrimidin-4-yl)amino)phenyl)acrylamide

    InChi Key: BFSRTTWIPACGMI-UHFFFAOYSA-N

    InChi Code: 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)

    SMILES Code: C=CC(NC1=CC=CC(NC2=NC(NC3=CC=C(NC4CN(CCF)C4)C=C3OC)=NC=C2C(F)(F)F)=C1)=O

    Synonyms

    CNX-2006; CNX 2006; CNX2006.


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    In Vitro

    In vitro activity: CNX-2006 is a novel irreversible EGFR tyrosine kinase inhibitor, specifically inhibits activating mutations of EGFR as well as the T790M mutation while having very weak inhibition at wild-type EGFR. In in vitro modeling of acquired resistance, continuous CNX-2006 treatment on drug-sensitive EGFR mutant cells leads to resistance more slowly than erlotinib. Dose escalation with CNX-2006 leads to differential effects in different lines, but does not select for T790M-mediated resistance. CNX-2006 resistent cells shows increased expression of EMT markers and MMP9.


    Kinase Assay: Human EGFR mutant lung adenocarcinoma cell lines are treated with drugs in standard growth inhibition assays. 


    Cell Assay: Cells with endogenous or transiently transfected mutant EGFRs (293 cells) are treated with inhibitors for 6 hours and then corresponding lysates are extracted and analyzed by immunoblotting.

    In VivoCNX-2006 is effective in H1975 (EGFR L858R/T790M) xenograft model.
    Animal modelNude mice
    Formulation & Dosage5% DMSO:15% Solutol HS15 in PBS; 25 mg/kg; i.p.
    ReferencesGalvani E, Sun J, Leon LG, et al.  Oncotarget, 2015.


    These protocols are for reference only. InvivoChem does not independently validate these methods.

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