Canertinib (dihydrochloride)

Canertinib dihydrochloride (CI-1033 dihydrochloride) is a potent and irreversible EGFR inhibitor; inhibits cellular EGFR and ErbB2 autophosphorylation with IC50s of 7.4 and 9 nM. Canertinib dihydrochloride is active against vaccinia virus respiratory infection in mice[1][2][3][4].

Product Specifications

CAS Number

[289499-45-2]

Product Name Alternative

CI-1033 dihydrochloride; PD-183805 dihydrochloride

UNSPSC

12352005

Hazard Statement

H315, H319, H335

Target

EGFR; Orthopoxvirus

Type

Reference compound

Related Pathways

Anti-infection; JAK/STAT Signaling; Protein Tyrosine Kinase/RTK

Applications

Cancer-Kinase/protease

Field of Research

Cancer; Infection

Assay Protocol

https://www.medchemexpress.com/Canertinib-dihydrochloride.html

Purity

99.68

Solubility

DMSO : 62.5 mg/mL (ultrasonic) |H2O : 25 mg/mL (ultrasonic)

Smiles

C=CC(NC1=CC2=C(N=CN=C2C=C1OCCCN3CCOCC3)NC4=CC=C(C(Cl)=C4)F)=O.[H]Cl.[H]Cl

Molecular Formula

C24H27Cl3FN5O3

Molecular Weight

558.86

Precautions

H315, H319, H335

References & Citations

[1]Smaill JB, et al. Tyrosine kinase inhibitors. 17. Irreversible inhibitors of the epidermal growth factor receptor: 4- (phenylamino) quinazoline- and 4- (phenylamino) pyrido[3,2-d]pyrimidine-6-acrylamides bearing additional solubilizing functions. J Med Chem. 2000 Apr 6;43 (7) :1380-97.|[2]Djerf Severinsson EA, et al. 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.|[3]McAndrews KM, et, al. Mechanisms associated with biogenesis of exosomes in cancer. Mol Cancer. 2019 Mar 30;18 (1) :52.|[4]Smee DF, et, al. Progress in the discovery of compounds inhibiting orthopoxviruses in animal models. Antivir Chem Chemother. 2008;19 (3) :115-24.