1. JAK/STAT Signaling
    Protein Tyrosine Kinase/RTK
  2. EGFR
  3. WZ8040

WZ8040 

Cat. No.: HY-12029
Handling Instructions

WZ8040 is an irreversible mutated EGFR T790M inhibitor and inhibits EGFR phosphorylation. WZ8040 displays 100-fold greater activity against the mutated EGFR than the normal.

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

WZ8040 Chemical Structure

WZ8040 Chemical Structure

CAS No. : 1214265-57-2

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Description

WZ8040 is an irreversible mutated EGFR T790M inhibitor and inhibits EGFR phosphorylation. WZ8040 displays 100-fold greater activity against the mutated EGFR than the normal[1].

IC50 & Target

EGFR Del E746_A750

1 nM (IC50, in HCC827 cells)

EGFR Del E746_A750

6 nM (IC50, in PC9 cells)

EGFR L858R

66 nM (IC50, in H3255 cells )

EGFR L858R/T790M

9 nM (IC50, in H1975 cells)

EGFR Del E746_A750/T790M

8 nM (IC50, in PC9 GR cells)

EGFR E746_A750/MET amp

>3.3 μM (IC50, in HCC827 GR cells)

ERBB2 amp

738 nM (IC50, in H1819 cells)

ERBB2 amp

915 nM (IC50, in Calu-3 cells)

ERBB2 Ins G776V, C

744 nM (IC50, in H1781 cells)

EGFR & ERBB2 WT

1.82 μM (IC50, in HN11 cells)

In Vitro

WZ8040 exhibits IC50 values of 1 nM for HCC827 (EGFR Del E746_A750), 6 nM for PC9 (EGFR Del E746_A750), 66 nM for H3255 (EGFR L858R), 9 nM for H1975 (EGFR L858R/T790M), 8 nM for PC9 GR (EGFR Del E746_A750/T790M), >3.3 μM for HCC827 GR (EGFR E746_A750/MET amp), 738 nM for H1819 (ERBB2 amp), 915 nM for Calu-3 (ERBB2 amp), 744 nM for H1781 (ERBB2 Ins G776V, C), 1.82 μM for HN11 (EGFR & ERBB2 WT), respectively[1].

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

Western Blot Analysis[1]

Cell Line: NSCLC cell lines and Ba/F3 cells.
Concentration: 0-3.3 μM.
Incubation Time: 24 hours.
Result: Exhibited activity for EGFR-mutated NSCLC lines, such as HH827, PC9, H3255, H1819, Calu-3, H1781 and HN11 cells.
Molecular Weight

481.01

Formula

C₂₄H₂₅ClN₆OS

CAS No.

1214265-57-2

SMILES

CN1CCN(C2=CC=C(C=C2)NC3=NC=C(C(SC4=CC(NC(C=C)=O)=CC=C4)=N3)Cl)CC1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
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Keywords:

WZ8040WZ 8040WZ-8040EGFREpidermal growth factor receptorErbB-1HER1mutatedphosphorylationNSCLCInhibitorinhibitorinhibit

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