Canertinib (CI-1033, PD-183805) | 1617

Canertinib is an irreversible tyrosine kinase inhibitor. It not only inhibits tyrosine phosphorylation but also enhances ubiquitinylation and accelerates endocytosis and subsequent intracellular destruction of ErbB-2 molecules. Canertinib alkylates a cysteine residue specific to ErbB receptors. The degradative pathway of ErbB receptor tyrosine kinases stimulated by tyrosine kinase inhibitors appears to be chaperone mediated, and thus is similar to the pathways activated by the heat shock protein 90 (Hsp90) antagonist geldanamycin and by stress-induced mechanisms.

Canertinib (CI-1033) is is an orally bioavailable irreversible Pan-erbB tyrosine kinase inhibitor, targeting EGFR with IC50 of 0.8, 19 and 7 nM for EGFR, HER-2 and ErbB-4, respectively.

1617 | Canertinib (CI-1033, PD-183805) DataSheet

Alternate Name/Synonyms: CI-1033, PD-183805, PD 183805

Appearance: Off-white to pale green solid

Formulation: N/A

CAS Number: 289499-45-2

Structure Available?: Yes

Peptide sequence: N/A

Salt Form: No

Molecular Formula: C₂₄H₂₅ClFN₅O₃ . 2HCl

Molecular Weight: 558.86

Cell-Permeable?: Yes

Purity: ≥99%

Solubilities: DMSO (100 mg/ml)

Handling: Protect from air and moisture

Country of Origin: USA

Tag Line: An ErbB receptor tyrosine kinase inhibitor

MDL Number: MFCD09954112

PubChem CID: 156413

SMILES: C=CC(=O)NC1=C(C=C2C(=C1)C(=NC=N2)NC3=CC(=C(C=C3)F)Cl)OCCCN4CCOCC4.Cl.Cl

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

InChi Key: JZZFDCXSFTVOJY-UHFFFAOYSA-N