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).[1][2] By 2015, Pfizer had discontinued development of the drug.[3]
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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
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Identifiers | |
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3D model (JSmol)
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ChEBI |
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ChEMBL |
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PubChem CID
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CompTox Dashboard (EPA)
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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).
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Infobox references
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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]