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CI 1033
- Canertinib dihydrochloride
- Parent CAS: 267243-28-7
- Soluble in water and DMSO
- MF: C24H25ClFN5O3.2HCl
- MW: 558.86
Description
CI 1033 (Canertinib) is an orally active and irreversible pan-ERBB receptor tyrosine kinase inhibitor that targets EGFR, HER2 and HER4.
Canertinib covalently suppresses ERBB receptor signaling, leading to sustained inhibition of MAPK and PI3K–AKT pathways. It is used to study irreversible kinase inhibition, HER-family dependence and mechanisms of resistance.
Key Features
- Irreversible pan-ERBB tyrosine kinase inhibitor
- Targets EGFR, HER2 and HER4
- Produces sustained suppression of ERBB signaling
- Orally active oncology pharmacology
Applications
- ERBB-family kinase assays
- EGFR/HER2-dependent cancer models
- Covalent inhibitor mechanism studies
- Drug-resistance and pathway-reactivation research
More Information
| Parent CAS No. | 267243-28-7 |
|---|---|
| Chemical Name | N-[4-(3-Chloro-4-fluoro-phenylamino)-7-(3-morpholin-4-yl-propoxy)-quinazolin-6-yl]-acrylamide dihydrochloride |
| SMILES | C1CN(CCCOC2C(NC(=O)C=C)=CC3=C(NC4C=CC(F)=C(Cl)C=4)N=CN=C3C=2)CCO1.Cl.Cl |
| MFCD | MFCD09954112 |
| 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 |
| CID | 156413 |
| Short Description | EGFR inhibitor |
References
- PA. Jänne et al. Multicenter, Randomized, Phase II Trial of CI-1033, an Irreversible Pan-ERBB Inhibitor, for Previously Treated Advanced Non–Small-Cell Lung Cancer. J. Clinic. Oncology, 2007, 25(25), 3936-3944.
- E Calvo et al. Administration of CI-1033, an Irreversible Pan-erbB Tyrosine Kinase Inhibitor, Is Feasible on a 7-Day On, 7-Day Off Schedule. A Phase I Pharmacokinetic and Food Effect Study. Clinical Cancer Research 2004, 10, 7112-7120.
- LV Sequist. Second-Generation Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitors in Non-Small Cell Lung Cancer. The Oncologist, 2007, 12(3), 325-330.
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