Canertinib

• CAT Number: I002916
• CAS Number: 267243-28-7
• Molecular Formula: C24H25ClFN5O3
• Molecular Weight: 485.94
• Purity: ≥95%
• Target: EGFR
• Solubility: DMSO ≥5.6mg/mL Water <1.2mg/mL Ethanol <1.2mg/
• Storage: 3 years -20C powder
• IC50: 0.8nM
• InChIKey: OMZCMEYTWSXEPZ-UHFFFAOYSA-N
• SMILES: C=CC(=O)NC1=C(C=C2C(=C1)C(=NC=N2)NC3=CC(=C(C=C3)F)Cl)OCCCN4CCOCC4

Canertinib (CAT: I002916) is a small molecule tyrosine kinase inhibitor that targets the epidermal growth factor receptor (EGFR) and human epidermal growth factor receptor 2 (HER2). It exerts its pharmacological activity by irreversibly inhibiting the kinase activity of EGFR and HER2, thereby interfering with signaling pathways involved in cell proliferation and survival. Canertinib has shown potential in the treatment of various types of cancers, including breast, lung, and colorectal cancers that overexpress EGFR or HER2. It is primarily used in combination with other chemotherapy agents to enhance the efficacy of cancer treatment.

Reference

1: Tang J, Qian Y, Li H, Kopecky BJ, Ding D, Ou HC, DeCook R, Chen X, Sun Z,
Kobel M, Bao J. Canertinib induces ototoxicity in three preclinical models. Hear
Res. 2015 Oct;328:59-66. doi: 10.1016/j.heares.2015.07.002. Epub 2015 Jul 7.
PubMed PMID: 26163095; PubMed Central PMCID: PMC4581429.

2: 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; PubMed
Central PMCID: PMC3573846.

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; PubMed Central PMCID: PMC3786202.

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. doi: 10.1016/j.bbrc.2011.05.148.
Epub 2011 Jun 6. PubMed PMID: 21669187.