Canertinib dihydrochloride is the hydrochloride salt of an orally bio-available quinazoline with potential antineoplastic and radiosensitizing activities. Canertinib binds to the intracellular domains of epidermal growth factor receptor tyrosine kinases (ErbB family), irreversibly inhibiting their signal transduction functions and resulting in tumor cell apoptosis and suppression of tumor cell proliferation. This agent also acts as a radiosensitizing agent and displays synergistic activity with other chemotherapeutic agents.
1: Minocha M, Khurana V, Qin B, Pal D, Mitra AK. Enhanced brain accumulation of pazopanib by modulating P-gp and Bcrp1 mediated efflux with canertinib or erlotinib. Int J Pharm. 2012 Oct 15;436(1-2):127-34. doi: 10.1016/j.ijpharm.2012.05.038. Epub 2012 Jun 9. PubMed PMID: 22688250.
2: Djerf Severinsson EA, Trinks C, Gréen H, Abdiu A, Hallbeck AL, Stål O, Walz TM. The pan-ErbB receptor tyrosine kinase inhibitor canertinib promotes apoptosis of malignant melanoma in vitro and displays anti-tumor activity in vivo. Biochem Biophys Res Commun. 2011 Oct 28;414(3):563-8. Epub 2011 Oct 1. PubMed PMID: 21982771.
3: Nordigården A, Zetterblad J, Trinks C, Gréen H, Eliasson P, Druid P, Lotfi K, Rönnstrand L, Walz TM, Jönsson JI. Irreversible pan-ERBB inhibitor canertinib elicits anti-leukaemic effects and induces the regression of FLT3-ITD transformed cells in mice. Br J Haematol. 2011 Oct;155(2):198-208. doi: 10.1111/j.1365-2141.2011.08819.x. Epub 2011 Aug 16. PubMed PMID: 21848891.
4: Prasasya RD, Vang KZ, Kreeger PK. A multivariate model of ErbB network composition predicts ovarian cancer cell response to canertinib. Biotechnol Bioeng. 2012 Jan;109(1):213-24. doi: 10.1002/bit.23297. Epub 2011 Aug 23. PubMed PMID: 21830205.
5: Trinks C, Severinsson EA, Holmlund B, Gréen A, Gréen H, Jönsson JI, Hallbeck AL, Walz TM. The pan-ErbB tyrosine kinase inhibitor canertinib induces caspase-mediated cell death in human T-cell leukemia (Jurkat) cells. Biochem Biophys Res Commun. 2011 Jul 8;410(3):422-7. Epub 2011 Jun 6. PubMed PMID: 21669187.
6: Trinks C, Djerf EA, Hallbeck AL, Jönsson JI, Walz TM. The pan-ErbB receptor tyrosine kinase inhibitor canertinib induces ErbB-independent apoptosis in human leukemia (HL-60 and U-937) cells. Biochem Biophys Res Commun. 2010 Feb 26;393(1):6-10. Epub 2010 Jan 22. PubMed PMID: 20096663.
7: Galmarini CM. Canertinib pfizer. IDrugs. 2004 Jan;7(1):58-63. Review. PubMed PMID: 14730468.
Chemical |
CAS Num |
289499-45-2 (HCl salt) |
Chemical Formula |
C24H27Cl3FN5O3 |
Molecular Weight |
558.86 |
IUPAC Chemical Name |
N-(4-((3-Chloro-4-fluorophenyl)amino)-7-(3-(morpholin-4-yl)propoxy)quinazolin-6-yl)prop-2-enamide |
Elemental Analysis |
C, 51.58; H, 4.87; Cl, 19.03; F, 3.40; N, 12.53; O, 8.59 |
Synonym |
CI1033PD183805. |
Solubility |
Soluble in DMSO, not in water |
SMILES Code |
C=CC(NC1=CC2=C(NC3=CC=C(F)C(Cl)=C3)N=CN=C2C=C1OCCCN4CCOCC4)=O |
Biological |
Targets and Effects |
epidermal growth factor (EGF) receptor kinase INHIBITOR |
Pathways |
Apoptosis |
Physical |
Appearance |
Solid powder |
Purity |
>98% (or refer to the Certificate of Analysis) |
Shipping Condition |
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs. |
Storage Condition |
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years). |
Shelf Life |
>5 years if stored properly |