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Canertinib | Covalent Inhibitor of EGFR, ERBB2
RATINGS:
Cellular Use: (1 reviews)

In Model Organisms: (0 reviews)
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
References
Vendors
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Probe Summary

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Targets Biochemical/Biophysical Potency Cellular Potency
EGFR
  • IC 50:1.5 nM EGFR
  • IC 50:7.4 nM
ERBB2
    • IC 50:9.0 nM
    Covalent Inhibitor
    up to 1 uM

    Selectivity

    In Cell Selectivity Assessment
    Potency Assay Off-Target:
    Using kinobead competition assays in breast cancer cells, a Science study identified canertinib as a ...

    Potency
    Cellular
    In Vitro

    EGFR

    Mode of Action: Covalent Inhibitor

    Structure-Activity-Relationship data available? Yes

    DOI Reference: 10.1021/jm990482t

    ERBB2

    Mode of Action: Covalent Inhibitor

    Structure-Activity-Relationship data available? No

    DOI Reference: 10.1021/jm990482t

    In Vivo Validations

    Mouse
    Dose: 20-80 mg/kg
    Route of delivery: Oral

    DOI Reference: 10.1021/jm990482t

    Orthogonal Probes def

    AFATINIB
    LAPATINIB
    SJF1528

    Chemical Information

    Molecular Formula C24H25ClFN5O3
    SMILEs C=CC(=O)Nc1cc2c(Nc3ccc(F)c(Cl)c3)ncnc2cc1OCCCN1CCOCC1
    InChI InChI=1S/C24H25ClFN5O3/c1-2-23(32)30-21-13-17-20(14-22(21)34-9-3-6-31-7-10-33-11-8-31)27-15-28-24(17)29-16-4-5-19(26)18(25)12-16/h2,4-5,12-15H,1,3,6-11H2,(H,30,32)(H,27,28,29)
    Molecular weight 485.16 Da
    AlogP 4.391500000000003
    HBond acceptors 8
    HBond donors 2
    Atoms 59

    Vendors

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    Expert Reviews

    by SERP+
    (on 9 Jul 2026)
    Cellular Use Rating
    Canertinib is a pan-inhibitor of the ErbB family with low nanomolar in vitro potency for all 4 family members. It is more potent for WT-EGFR than mutant EGFR. It is not particularly selective within the...
    Note: The Chemical Probes Portal only endorses compounds as chemical probes for use as specific and selective modulators of the proposed target if they receive three or more (3-4) stars. Read more about our evaluation criteria