| 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 |
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| UNII | |
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| Properties | |
| C24H25ClFN5O3 | |
| Molar mass | 485.94 g·mol−1 |
Except where otherwise noted, data are given for materials in theirstandard state (at 25 °C [77 °F], 100 kPa). | |
Canertinib (CI-1033) is an experimental drug candidate for the treatment of cancer. It is anirreversibletyrosine-kinase inhibitor with activity againstEGFR (IC50 0.8 nM),HER-2 (IC50 19 nM) andErbB-4 (IC50 7 nM).[1][2] By 2015, Pfizer had discontinued development of the drug.[3]
Canertinib has been reported as a substrate for the transporter proteinOATP1B3. 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 theOATP1B1 or OATP1B3 transporters.[5]
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