Canertinib (CI-1033, PD-183805)

• CAT Number: I002998
• CAS Number: 289499-45-2
• Molecular Formula: C₂₄H₂₅ClFN₅O₃ . 2HCl
• Molecular Weight: 558.86
• Purity: ≥95%
• Synonyms: N-[4-(3-chloro-4-fluoroanilino)-7-(3-morpholin-4-ylpropoxy)quinazolin-6-yl]prop-2-enamide;dihydrochloride
• Target: Protein Tyrosine Kinase/RTK
• Solubility: DMSO:>10 mg/mL; water: >10 mg/mL
• Storage: Store at -20°C
• IC50: 1.5/0.9 nM(EGFR/ErbB2)
• InChI: InChI=1S/C24H25ClFN5O3.2ClH/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);2*1H
• InChIKey: JZZFDCXSFTVOJY-UHFFFAOYSA-N
• SMILES: C=CC(=O)NC1=C(C=C2C(=C1)C(=NC=N2)NC3=CC(=C(C=C3)F)Cl)OCCCN4CCOCC4.Cl.Cl

Canertinib (CI-1033, PD-183805) is an irreversible tyrosine kinase inhibitor targeting the epidermal growth factor receptor (EGFR) and other ErbB family receptors. By binding to the ATP-binding site, it prevents receptor phosphorylation, thereby inhibiting downstream signaling pathways critical for cell proliferation and survival. Canertinib has shown potential in treating various cancers, including non-small cell lung cancer (NSCLC) and breast cancer. Its selective inhibition of ErbB receptors makes it a promising candidate for targeted cancer therapy.