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    InvivoChem Cat #: V0566
    CAS #: 1214265-57-2Purity ≥98%

    Description: WZ8040 is a novel, potent, mutant-selective and covalent / irreversible EGFR(T790M) inhibitor with potential anticancer activity, it does not inhibit the phosphorylation of ERBB2 (T798I). 

    References: Nature. 2009 Dec 24;462(7276):1070-4.

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    Molecular Weight (MW)481.01
    CAS No.1214265-57-2
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 96 mg/mL (199.6 mM)
    Water: <1 mg/mL
    Ethanol: 3 mg/mL (6.2 mM) 
    Other infoChemical Name: N-(3-((5-chloro-2-((4-(4-methylpiperazin-1-yl)phenyl)amino)pyrimidin-4-yl)thio)phenyl)acrylamide
    InChi Code: InChI=1S/C24H25ClN6OS/c1-3-22(32)27-18-5-4-6-20(15-18)33-23-21(25)16-26-24(29-23)28-17-7-9-19(10-8-17)31-13-11-30(2)12-14-31/h3-10,15-16H,1,11-14H2,2H3,(H,27,32)(H,26,28,29)
    SMILES Code: C=CC(NC1=CC=CC(SC2=NC(NC3=CC=C(N4CCN(C)CC4)C=C3)=NC=C2Cl)=C1)=O 
    SynonymsWZ8040; WZ 8040; WZ8040; 

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    In Vitro

    In vitro activity: WZ8040 is 30- to 100-fold more potent against EGFR T790M, and up to 100-fold less potent against wild-type EGFR, than quinazoline-based EGFR inhibitors such as CL-387785 and HKI-272. WZ8040 treatment potently inhibits the growth of HCC827 (EGFR Del E746_A750), PC9 (EGFR Del E746_A750), H3255 (EGFR L858R), H1975 (EGFR L858R/T790M), and PC9 GR (EGFR Del E746_A750/T790M) with IC50 of 1 nM, 6 nM, 66 nM, 9 nM, and 8 nM, respectively. WZ8040 weakly inhibits the growth of HCC827 GR (EGFR E746_A750/MET amp), H1819 (ERBB2 amp), Calu-3 (ERBB2 amp), H1781 (ERBB2 Ins G776V, C), and HN11 (EGFR & ERBB2 WT) with IC50 of >3.3 μM, 738 nM, 915 nM, 744 nM, and 1.82 μM, respectively. WZ8040 is not toxic up to 10 μM against A549 (KRAS mutant) or H3122 (EML4-ALK) cells.

    Cell Assay: Cells (HCC827, H3255, HCC827 GR, H1975, PC9, PC9 GR, Calu-3, H1819, and Ba/F3) are exposed to increasing concentrations of WZ8040 for 72 hours. Growth is assessed using the MTS survival assay.

    In VivoWZ4002 inhibits EGFR phosphorylation and induces significant tumor regression in murine models of EGFR T790M. 
    Animal modelMurine models of EGFR T790M
    Formulation & Dosage
    ReferencesNature. 2009 Dec 24;462(7276):1070-4.

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


    WZ4002, WZ3146 and WZ8040 are novel EGFR inhibitors, suppress the growth of EGFR T790M containing cell lines and inhibit EGFR phosphorylation. Nature. 2009 Dec 24; 462(7276): 1070–1074.


    WZ4002 is less potent than quinazoline EGFR inhibitors against wild type EGFR in vitro and in vivo. Nature. 2009 Dec 24; 462(7276): 1070–1074.


    WZ4002 inhibits EGFR phosphorylation and induces significant tumor regression in murine models of EGFR T790M. Nature. 2009 Dec 24; 462(7276): 1070–1074.


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