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    WZ4002
    WZ4002

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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 #: V0552
    CAS #: 1213269-23-8Purity ≥98%

    Description: WZ4002 (WZ-4002) is a covalent/irreversible and mutant-selective EGFR (e.g. L858R/T790M) inhibitor with potential antitumor activity. It inhibits EGFR(L858R)/(T790M) with IC50s of 2 nM/8 nM in BaF3 cell line. 

    References: Nature. 2009 Dec 24;462(7276):1070-4; J Nucl Med. 2012 Mar;53(3):443-50.

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    Molecular Weight (MW)494.18
    FormulaC25H27ClN6O3
    CAS No.1213269-23-8
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 13 mg/mL (26.3 mM)
    Water: <1 mg/mL
    Ethanol: <1 mg/mL
    Solubility (In vivo)30% PEG400+0.5% Tween80+5% propylene glycol: 30 mg/mL 
    Synonyms

    Synonym: WZ-4002; WZ 4002; WZ4002;

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

    InChi Key: ITTRLTNMFYIYPA-UHFFFAOYSA-N

    InChi Code: InChI=1S/C25H27ClN6O3/c1-4-23(33)28-17-6-5-7-19(14-17)35-24-20(26)16-27-25(30-24)29-21-9-8-18(15-22(21)34-3)32-12-10-31(2)11-13-32/h4-9,14-16H,1,10-13H2,2-3H3,(H,28,33)(H,27,29,30)

    SMILES Code: C=CC(NC1=CC=CC(OC2=NC(NC3=CC=C(N4CCN(C)CC4)C=C3OC)=NC=C2Cl)=C1)=O


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    In Vitro

    In vitro activity: WZ4002 inhibits other EGFR genotypes E746_A750 and E746_A750/T790M with IC50 of 2 and 6 nM. Besides, WZ4002 suppresses widetype ERBB2 with an IC50 of 32 nM. WZ4002 inhibits EGFR, AKT and ERK1/2 phosphorylation in NSCLC cell lines and WZ4002 prevents of EGFR phosphorylation in NIH-3T3 cells expressing different EGFR T790M mutant alleles. For WZ4002, kinases that exhibited greater than 95% inhibition relative to the DMSO control at 10 μM are selected for measurement of their dissociation constants. WZ4002, which possesses an ortho-methoxy group at the C2-aniline substituent, is more selective for EGFR compared to WZ3146. WZ4002 is 100-fold less effective at inhibiting phosphorylation of WT EGFR compared to the quinazoline inhibitors. Similarly, WZ4002 prevents EGFR kinase activity of recombinant L858R/T790M protein more potently than of WT EGFR, while the opposite is observed with HKI-272 and gefitinib. In addition, the phosphorylated EGFR of Src TKI-resistant H1975 cells, as well as HCC827 cells, is completely suppressed by the third generation EGFR TKI, WZ4002.


    Kinase Assay: In vitro inhibitory enzyme kinetic assays using recombinant EGFR L858R/T790M and WT protein and are performed using the ATP/NADH coupled assay system in a 96-well format. WZ4002 is added to determine its inhibitory effects.


    Cell Assay: The NSCLC, Ba/F3 cells, NIH-3T3 cells, PC9GR4 cells are used and verified to contain EGFR delE746_A750/T790M by direct sequencing. Cell proliferation and growth assays are performed using the MTS assay. Site directed mutagenesis is performed using the Quick Change Site-Directed Mutagenesis kit.

    In VivoIn a 2-week efficacy study, WZ4002 treatment results in significant tumor regressions compared to vehicle alone in both T790M containing murine models. Treatment with low-dose WZ4002, and high-dose WZ4002 leads to mean decreases in tracer uptake of 26%, and 36%, respectively.
    Animal modelEGFR-TL (T790M/L858R) mice
    Formulation & DosageDissolved in NMP (10% 1-methyl-2-pyrrolidinone: 90% PEG-300;  25 mg/kg; Oral gavage
    References

    Nature. 2009 Dec 24;462(7276):1070-4; J Nucl Med. 2012 Mar;53(3):443-50.


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

    WZ4002

    WZ4002


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