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Abandoned drugs
Canertinib
Другие языки:

    Canertinib

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    Canertinib
    Canertinib.svg
    Names
    Preferred IUPAC name
    N-{4-(3-Chloro-4-fluoroanilino)-7-[3-(morpholin-4-yl)propoxy]quinazolin-6-yl}prop-2-enamide
    Other names
    CI-1033; PD-183805
    Identifiers
    3D model (JSmol)
    ChEBI
    ChEMBL
    ChemSpider
    PubChem CID
    UNII
    • 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) checkY
      Key: OMZCMEYTWSXEPZ-UHFFFAOYSA-N checkY
    • InChI=1/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)
      Key: OMZCMEYTWSXEPZ-UHFFFAOYAG
    • Fc1ccc(cc1Cl)Nc4ncnc3cc(OCCCN2CCOCC2)c(NC(=O)\C=C)cc34
    Properties
    C24H25ClFN5O3
    Molar mass 485.94 g·mol−1
    Except where otherwise noted, data are given for materials in their standard state (at 25 °C [77 °F], 100 kPa).
    ☒N verify (what is checkY☒N ?)

    Canertinib (CI-1033) is an experimental drug candidate for the treatment of cancer. It is an irreversible tyrosine-kinase inhibitor with activity against EGFR (IC50 0.8 nM), HER-2 (IC50 19 nM) and ErbB-4 (IC50 7 nM). By 2015, Pfizer had discontinued development of the drug.

    Canertinib has been reported as a substrate for the transporter protein OATP1B3. Interaction of canertinib with OATP1B3 may alter its hepatic disposition and can lead to transporter mediated drug-drug interactions. Canertinib is not an inhibitor of the OATP1B1 or OATP1B3 transporters.



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