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Icotinib Hydrochloride

CAS No. 1204313-51-8

Icotinib Hydrochloride( BPI-2009H )

Catalog No. M17189 CAS No. 1204313-51-8

Icotinib Hydrochloride is the hydrochloride salt form of icotinib, an orally available quinazoline-based inhibitor of EGFR, with potential antineoplastic activity.

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
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Biological Information

  • Product Name
    Icotinib Hydrochloride
  • Note
    Research use only, not for human use.
  • Brief Description
    Icotinib Hydrochloride is the hydrochloride salt form of icotinib, an orally available quinazoline-based inhibitor of EGFR, with potential antineoplastic activity.
  • Description
    Icotinib Hydrochloride is the hydrochloride salt form of icotinib, an orally available quinazoline-based inhibitor of EGFR, with potential antineoplastic activity. Icotinib selectively inhibits the wild-type and several mutated forms of EGFR tyrosine kinase. This may lead to an inhibition of EGFR-mediated signal transduction and may inhibit cancer cell proliferation. EGFR, a receptor tyrosine kinase, has been upregulated in a variety of cancer cell types.
  • In Vitro
    Incubation with Iconitib at 0.5 μM results in kinase activity inhibition of 91%, 99%, 96%, 61% and 61%, respectively. Iconitib inhibits the proliferation of A431 and BGC-823 A549, H460 and KB cell lines with IC50s of 1, 4.06, 12.16, 16.08, 40.71 μM. When profiled with 88 kinases, Icotinib only shows meaningful inhibitory activity to EGFR and its mutants. Icotinib blocks EGFR-mediated intracellular tyrosine phosphorylation (IC50=45 nM) in the human epidermoid carcinoma A431 cell line and inhibits tumor cell proliferation.
  • In Vivo
    Icotinib exhibits potent dose-dependent antitumor effects in nude mice carrying a variety of human tumor-derived xenografts. The drug is well tolerated at doses up to 120 mg/kg/day in mice without mortality or significant body weight loss during the treatment. Icotinib inhibits tumor growth at a rate of 25.2%, 45.6% and 51.5% in the A431 cell line groups; 3.4%, 25.9% and 31.0% in the A549 cell line groups; 49.4%, 52.6% and 67.4% in the H460 cell line groups, and 30.3%, 36.4% and 46.5% in the HCT8 cell line groups, at 30, 60 and 120 mg/kg/dose, respectively.
  • Synonyms
    BPI-2009H
  • Pathway
    Others
  • Target
    Other Targets
  • Recptor
    EGFR| EGFR mutants
  • Research Area
    Cancer
  • Indication
    ——

Chemical Information

  • CAS Number
    1204313-51-8
  • Formula Weight
    427.88
  • Molecular Formula
    C22H22ClN3O4
  • Purity
    >98% (HPLC)
  • Solubility
    DMSO : 25 mg/mL. 58.43 mM;
  • SMILES
    C#Cc1cc(ccc1)Nc1ncnc2cc3OCCOCCOCCOc3cc12.Cl
  • Chemical Name
    ——

Shipping & Storage Information

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

Reference

1. Tan F, et al. Lung Y. 2012 May;76(2):177-82.
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