An inhibitor of mutant EGFR
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WZ3146

Item No. 23440

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[3-[[5-chloro-2-[[4-(4-methyl-1-piperazinyl)phenyl]amino]-4-pyrimidinyl]oxy]phenyl]-2-propenamide
CAS Number
1214265-56-1
Molecular Formula
C24H25ClN6O2
Formula Weight
465.0
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMSO: 30 mg/mlEthanol: 30 mg/mlEthanol:PBS (pH 7.2) (1:3): 0.25 mg/ml
λmax
287 nm
SMILES
CN1CCN(C2=CC=C(NC3=NC=C(Cl)C(OC4=CC=CC(NC(C=C)=O)=C4)=N3)C=C2)CC1
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)
InChi Key
APHGZZPEOCCYNO-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $49

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    5 mg

    $213

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    10 mg

    $376

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    50 mg

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    Product Description

    WZ3146 is an irreversible inhibitor of mutant EGF receptors (EGFRs) with IC50 values ranging from 2 to 2,740 nM in Ba/F3 cells.1 It is selective for EGFR mutants including EGFRL858R and EGFRDel E746_A750 (IC50s = 2 nM for both) over wild-type EGFR (IC50 = 750 nM in HN11 cells) but also inhibits ERBB2Ins G776V,C and wild-type ERBB2 (IC50s = 10 and 24 nM, respectively, in Ba/F3 cells). However, it does not inhibit the ERBB2T7981 gatekeeper mutant. WZ3146 (10-1,000 nM) decreases phosphorylation of EGFR, AKT, and ERK1/2 in H1975 non-small cell lung cancer (NSCLC) cells in a concentration-dependent manner. It inhibits proliferation of PC-9 NSCLC and gefitinib-resistant PC-9 GR cells (EC50s = 15 and 3 nM, respectively).2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Zhou, W., Ercan, D., Chen, L., et al. Novel mutant-selective EGFR kinase inhibitors against EGFR T790M. Nature 462(7276), 1070-1074 (2009).

    2. Zhou, W., Ercan, D., Jänne, P.A., et al. Discovery of selective irreversible inhibitors for EGFR-T790M. Bioorg. Med. Chem. Lett. 21(2), 638-643 (2011).