1. JAK/STAT Signaling
    Protein Tyrosine Kinase/RTK
  2. EGFR

WZ4002 

Cat. No.: HY-12026 Purity: 98.67%
Handling Instructions

WZ4002 is a mutant selective EGFR inhibitor with IC50s of 2, 8, 3 and 2 nM for EGFRL858R, EGFRL858R/T790M, EGFRE746_A750 and EGFRE746_A750/T790M, respectively.

For research use only. We do not sell to patients.

WZ4002 Chemical Structure

WZ4002 Chemical Structure

CAS No. : 1213269-23-8

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 92 In-stock
Estimated Time of Arrival: December 31
10 mg USD 84 In-stock
Estimated Time of Arrival: December 31
50 mg USD 240 In-stock
Estimated Time of Arrival: December 31
100 mg USD 420 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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    WZ4002 purchased from MCE. Usage Cited in: Oncotarget. 2015 Oct 13;6(31):31313-22.

    Effect of Ibrutinib on EGFR wt/mutant NSCLCs. Ibrutinib effects on wt EGFR and mutant EGFR- mediated signaling pathways. The results demonstrate that Ibrutinib potently inhibits both EGFR wt/mutant auto-phosphorylation at Y1068.

    WZ4002 purchased from MCE. Usage Cited in: Oncotarget. 2015 Oct 13;6(31):31313-22.

    Effect of Ibrutinib, WZ4002, AZD9291 and CO1686 on EGFR phosphorylation of tyrosines 1068 and 1173 in EGFR-dependent cancer cell lines.

    WZ4002 purchased from MCE. Usage Cited in: Oncotarget. 2016 Oct 25;7(43):69760-69769.

    Ibrutinib and WZ4002 inhibitory effects on EGFRY1068 auto-phosphorylation in the H1975 cell line at different time points by removal of drug after 4 h pretreatment
    • Biological Activity

    • Protocol

    • Technical Information

    • Purity & Documentation

    • References

    Description

    WZ4002 is a mutant selective EGFR inhibitor with IC50s of 2, 8, 3 and 2 nM for EGFRL858R, EGFRL858R/T790M, EGFRE746_A750 and EGFRE746_A750/T790M, respectively.

    IC50 & Target[1]

    EGFRL858R

    2 nM (IC50, Cell Assay)

    EGFRL858R/T790M

    8 nM (IC50, Cell Assay)

    EGFRE746_A750

    3 nM (IC50, Cell Assay)

    EGFRE746_A750/T790M

    2 nM (IC50, Cell Assay)

    In Vitro

    WZ4002 increases cellular potency correlated with inhibition of EGFR, AKT and ERK1/2 phosphorylation in NSCLC cell lines and EGFR phosphorylation in NIH-3T3 cells expressing different EGFRT790M mutant alleles. WZ4002 inhibits EGFR kinase activity of recombinant L858R/T790M protein more potently than of WT EGFR[1].

    In Vivo

    In a pharmacodynamic study WZ4002 effectively inhibits EGFR, AKT and ERK1/2 phosphorylation which is associated with a significant increase in TUNEL positive and a significant decrease in Ki67 positive cells compared to vehicle alone treated mice. In a 2 week efficacy study, WZ4002 treatment results in significant tumor regressions compared to vehicle alone in both T790M containing murine models. Histological evaluation of the lungs following treatment confirms significant resolution of the tumor nodules with only few small residual nodules and nodule remnants that has evidence of treatment effect with decreased cellularity and increased fibrosis consistent with remodeling/scarring[1].

    Solvent & Solubility
    In Vitro: 

    10 mM in DMSO

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.0203 mL 10.1016 mL 20.2032 mL
    5 mM 0.4041 mL 2.0203 mL 4.0406 mL
    10 mM 0.2020 mL 1.0102 mL 2.0203 mL
    *Please refer to the solubility information to select the appropriate solvent.
    References
    Kinase Assay
    [1]

    EGFR kinase assay is performed using a GST-kinase fusion protein. The final reaction mixture contained 60 mM HEPES pH 7.5, 5 mM MgCl2, 5 mM MnCl2, 3 mM Na3V04, 1.25 mM DTT, 20 μM ATP, 1.5 μM PTP1B (Tyr66) biotinylated peptide and 50 ng of EGFR kinase. A phospotyrosine mab (pTyr100) is used to detect phosphorylation of the EGFR substrate peptide in the presence of WZ4002, gefitinib or HKI-272 (concentration ranges 0-10 μM for all drugs) followed a fluorescent Anti-mouse IgG secondary antibody. Fluorescence emission is detected at 615 nm[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Cell Assay
    [1]

    Growth and inhibition of growth is assessed by MTS assay. Ba/F3 cells are exposed to WZ4002 treatment for 72 hours. Growth and inhibition of growth is assessed by MTS assay[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Administration
    [1]

    Cohorts of EGFR TL/CCSP-rtTA and EGFR TD/CCSP-rtTA are put on doxycycline diet at 5 weeks of age to induce the expression of mutant EGFR. These mice undergo MRI after 6 to 8 weeks of doxycycline diet to document and quantify the lung cancer burden before being assigned to various treatment study cohorts. There is a minimum of 3 mice per treatment group. Mice are then treated either with vehicle (NMP 13 (10% 1-methyl-2-pyrrolidinone: 90% PEG-300) alone or WZ4002 at 25mg/kg gavage daily. After 2 weeks of treatment, these mice undergo a second round of MRI to document their response to the treatment. MRIs and tumor burden measurement are performed[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    References
    Molecular Weight

    494.97

    Formula

    C₂₅H₂₇ClN₆O₃

    CAS No.

    1213269-23-8

    SMILES

    COC1=C(C=CC(N2CCN(CC2)C)=C1)NC3=NC=C(C(OC4=CC(NC(C=C)=O)=CC=C4)=N3)Cl

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Shipping

    Room temperature in continental US; may vary elsewhere

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    Product Name:
    WZ4002
    Cat. No.:
    HY-12026
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    WZ4002

    Cat. No.: HY-12026