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    WZ3146
    WZ3146

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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 #: V0565
    CAS #: 1214265-56-1Purity ≥98%

    Description: WZ3146 (WZ-3146) is a covalent / irreversible and mutant-selective inhibitor of EGFR (L858R and E746_A750) with potential anticancer activity. It inhibits EGFR (L858R and E746_A750) with IC50s of 2 nM and 2 nM, respectively; shows no effects on ERBB2 phosphorylation (T798I). WZ3146 exhibits potent anti-proliferative activity in vitro against EGFR T790M containing cell lines. 

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

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    Molecular Weight (MW)464.95
    FormulaC24H25ClN6O2
    CAS No.1214265-56-1
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 93 mg/mL (200.0 mM)
    Water: <1 mg/mL
    Ethanol: <1 mg/mL
    Solubility (In vivo)

    Chemical Name: N-(3-((5-chloro-2-((4-(4-methylpiperazin-1-yl)phenyl)amino)pyrimidin-4-yl)oxy)phenyl)acrylamide

    InChi Key: APHGZZPEOCCYNO-UHFFFAOYSA-N

    InChi Code: InChI=1S/C24H25ClN6O2/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(OC2=NC(NC3=CC=C(N4CCN(C)CC4)C=C3)=NC=C2Cl)=C1)=O

    Synonyms

    WZ-3146; WZ 3146; WZ3146; 


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    In Vitro

    In vitro activity: WZ3146 significantly suppresses the growth of EGFR mutation containing cell lines with IC50 of 3 nM in EGFR Del E746_A750 containing HCC827 cells, 15 nM in EGFR Del E746_A750 containing PC9 cells, 29 nM in EGFR L858R/T790M containing H1975 cells and 3 nM in EGFR Del E746_A750/T790M containing PC9 GR cells.


    Kinase Assay: The assays are carried out in triplicate using the ATP/NADH coupled assay system in a 96-well format. The final reaction mixture contains 0.5 mg/mL Bovine Serum Albumin (BSA), 2 mM MnCl2, 1 mM phospho(enol) pyruvic acid (PEP), 1 mM TCEP, 0.1 M Hepes 7.4, 2.5 mM poly-[Glu4Tyr1] peptide, 1/50 of the final reaction mixture volume of pyruvate kinase/lactic dehydrogenase enzymes from rabbit muscle, 0.5 mM NADH, 0.5 μM EGFR kinase, 100 μM ATP and varied amount of WZ3146. WZ3146 and ATP are mixed and made separate stock from the mixture with all other ingredients and added last to the latter to start the reaction. Steady state initial velocity data are drawn from the slopes of the A340 curves. 


    Cell Assay: Growth and inhibition of growth is assessed by MTS assay. NSCLC or Ba/F3 cells are exposed to treatment for 72 hours and the number of cells used per experiment is determined empirically. All experimental points are set up in six to twelve wells and all experiments are repeated at least three times. The data is graphically displayed using GraphPad Prism version 5.0 for Windows. The curves are fitted using a non-linear regression model with a sigmoidal dose response.

    In VivoWZ4002 inhibits EGFR phosphorylation and induces significant tumor regression in murine models of EGFR T790M.  
    Animal modelMurine models of EGFR T790M.
    Formulation & Dosage
    References

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


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

    WZ3146

    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.

    WZ3146

    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.

    WZ3146

    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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