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

WZ8040 

Cat. No.: HY-12029
Handling Instructions

WZ8040 is a novel mutant-selective irreversible EGFRT790M inhibitor, does not inhibit ERBB2 phosphorylation (T798I).

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 a novel mutant-selective irreversible EGFRT790M inhibitor, does not inhibit ERBB2 phosphorylation (T798I). IC50 value: Target: EGFRT790M 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.

Storage

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

References
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

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Room temperature in continental US; may vary elsewhere

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WZ8040
Cat. No.:
HY-12029
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Cat. No.: HY-12029