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1 References  














Canertinib






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From Wikipedia, the free encyclopedia
 


Canertinib
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

CAS Number

3D model (JSmol)

ChEBI
ChEMBL
  • ChEMBL545315 ☒N
  • ChemSpider

    IUPHAR/BPS

    PubChem CID

    UNII

    CompTox Dashboard (EPA)

    • 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

    Chemical formula

    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 ?)

    Infobox references

    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 (IC50nM).[1][2] By 2015, Pfizer had discontinued development of the drug.[3]

    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.[4] Canertinib is not an inhibitor of the OATP1B1 or OATP1B3 transporters.[5]

    References

    [edit]
    1. ^ Smaill, JB; Rewcastle, GW; Loo, JA; Greis, KD; Chan, OH; Reyner, EL; Lipka, E; Showalter, HD; et al. (2000). "Tyrosine kinase inhibitors. 17. Irreversible inhibitors of the epidermal growth factor receptor: 4-(phenylamino)quinazoline- and 4-(phenylamino)pyrido3,2-dpyrimidine-6-acrylamides bearing additional solubilizing functions". Journal of Medicinal Chemistry. 43 (7): 1380–97. doi:10.1021/jm990482t. PMID 10753475.
  • ^ CI-1033 (Canertinib), Selleck Chemicals
  • ^ "Canertinib - AdisInsight".
  • ^ Khurana V, Minocha M, Pal D, Mitra AK (March 2014). "Role of OATP-1B1 and/or OATP-1B3 in hepatic disposition of tyrosine kinase inhibitors". Drug Metabol Drug Interact. 29 (3): 179–90. doi:10.1515/dmdi-2013-0062. PMC 4407685. PMID 24643910.
  • ^ Khurana V, Minocha M, Pal D, Mitra AK (May 2014). "Inhibition of OATP-1B1 and OATP-1B3 by tyrosine kinase inhibitors". Drug Metabol Drug Interact. 29 (4): 249–59. doi:10.1515/dmdi-2014-0014. PMC 4407688. PMID 24807167.

  • t
  • e

  • Retrieved from "https://en.wikipedia.org/w/index.php?title=Canertinib&oldid=1217766686"

    Categories: 
    Acrylamides
    Tyrosine kinase inhibitors
    Quinazolines
    4-Morpholinyl compounds
    Fluoroarenes
    Chloroarenes
    Experimental cancer drugs
    Abandoned drugs
    Drugs developed by Pfizer
    Antineoplastic and immunomodulating drug stubs
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    This page was last edited on 7 April 2024, at 19:23 (UTC).

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