A pan-ErbB tyrosine kinase inhibitor
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Canertinib (hydrochloride)

Item No. 12076

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[4-[(3-chloro-4-fluorophenyl)amino]-7-[3-(4-morpholinyl)propoxy]-6-quinazolinyl]-2-propenamide, dihydrochloride
CAS Number
289499-45-2
Synonyms
  • CI-1033
  • PD 183805
Molecular Formula
C24H25ClFN5O3 • 2HCl
Formula Weight
558.9
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 14 mg/mlDMF:PBS(pH 7.2)(1:1): 0.5 mg/mlDMSO: 10 mg/ml
λmax
225, 257, 345 nm
SMILES
ClC1=C(F)C=CC(NC2=NC=NC3=C2C=C(NC(C=C)=O)C(OCCCN4CCOCC4)=C3)=C1.Cl.Cl
InChi Code
InChI=1S/C24H25ClFN5O3.2ClH/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);2*1H
InChi Key
JZZFDCXSFTVOJY-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $41

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    10 mg

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    25 mg

    $148

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    50 mg

    $274

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    Product Description

    Canertinib is an irreversible quinazoline-based HER family tyrosine kinase inhibitor with IC50 values of 0.8, 19, and 7 nM for blocking in vitro activity of EGFR, HER2, and HER4, respectively.1 As a broadly applicable anti-cancer agent, it has been used to suppress proliferation of malignant peripheral nerve sheath tumor cells (effective concentration of 250-500 nM), to inhibit growth and induce dose-dependent apoptosis in a panel of neuroblastoma cell lines (IC50s = 0.94-2.45 μM), and to reduce proliferation of acute myeloid leukemia cells (IC50 = 0.27 μM).2,3,4 Canertinib also displays anti-neoplastic activity towards T98G glioblastoma cells, HCT8 colorectal carcinoma cells, and cells expressing the breast cancer resistance protein.5

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Arkin, M., and Moasser, M.M. HER2 directed small molecule antagonists. Curr. Opin. Investig. Drugs 9(12), 1264-1276 (2008).

    2. Dilworth, J.T., Wojtkowiak, J.W., Mathieu, P., et al. Suppression of proliferation of two independent NF1 malignant peripheral nerve sheath tumor cell lines by the pan-ErbB inhibitor Cl-1033. Cancer Biol. Ther. 7(12), 1938-1946 (2008).

    3. Richards, K.N., Zweidler-McKay, P.A., Van Roy, N., et al. Signaling of ERBB receptor tyrosine kinases promotes neuroblastoma growth in vitro and in vivo. Cancer 116(13), 3233-3243 (2010).

    4. Nordigården, A., Zetterblad, J., Trinks, C., et al. Irreversible pan-ERBB inhibitor canertinib elicits anti-leukaemic effects and induces the regression of FLT3-ITD transformed cells in mice. Br. J. Haematol. 155, 198-208 (2011).

    5. Erlichman, C., Boerner, S.A., Hallgren, C.G., et al. The HER tyrosine kinase inhibitor CI1033 enhances cytotoxicity of 7-ethyl-10-hydroxycamptothecin and topotecan by inhibiting breast cancer resistance protein-mediated drug efflux. Cancer Res. 61, 739-748 (2001).