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Canertinib dihydrochloride

CAS No. 289499-45-2

Canertinib dihydrochloride ( Canertinib;CI-1033 dihydrochloride;PD-183805 dihydrochloride;CI1033 dihydrochloride )

Catalog No. M13886 CAS No. 289499-45-2

A potent, irreversible, orally available pan-ErbB inhibitor for EGFR and ErbB2 with IC50 of 7.5 nM and 9.0 nM in autophosphorylation assay.

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
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Biological Information

  • Product Name
    Canertinib dihydrochloride
  • Note
    Research use only, not for human use.
  • Brief Description
    A potent, irreversible, orally available pan-ErbB inhibitor for EGFR and ErbB2 with IC50 of 7.5 nM and 9.0 nM in autophosphorylation assay.
  • Description
    A potent, irreversible, orally available pan-ErbB inhibitor for EGFR and ErbB2 with IC50 of 7.5 nM and 9.0 nM in autophosphorylation assay; displays no activity to PDGFR, FGFR, InsR, PKC, and CDK1/2/4; suppresses heregulin-stimulated tyrosine phosphorylation of erbB2, erbB3 and erbB4 with IC50 of 5, 14 and 10 nM, respectively, also inhibits expression of pp62c-fos in response to heregulin; shows high in vivo activity against A431 xenografts.Lung Cancer Discontinued
  • Synonyms
    Canertinib;CI-1033 dihydrochloride;PD-183805 dihydrochloride;CI1033 dihydrochloride
  • Pathway
    Angiogenesis
  • Target
    EGFR
  • Recptor
    EGFR;HER2/ErbB2
  • Research Area
    Cancer
  • Indication
    Lung Cancer

Chemical Information

  • CAS Number
    289499-45-2
  • Formula Weight
    558.86
  • Molecular Formula
    C24H27Cl3FN5O3
  • Purity
    >98% (HPLC)
  • Solubility
    10 mM in DMSO
  • SMILES
    C=CC(=O)NC1=C(C=C2C(=C1)C(=NC=N2)NC3=CC(=C(C=C3)F)Cl)OCCCN4CCOCC4.Cl.Cl
  • Chemical Name
    2-Propenamide, N-[4-[(3-chloro-4-fluorophenyl)amino]-7-[3-(4-morpholinyl)propoxy]-6-quinazolinyl]-, hydrochloride (1:2)

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

1. Smaill JB, et al. J Med Chem. 2000 Apr 6;43(7):1380-97.
2. Erlichman C, et al. Cancer Res. 2001 Jan 15;61(2):739-48.
3. Nyati MK, et al. Clin Cancer Res. 2004 Jan 15;10(2):691-700.
4. Slichenmyer WJ, et al. Semin Oncol. 2001 Oct;28(5 Suppl 16):80-5.
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