Canertinib (dihydrochloride)

• UNSPSC Description:

  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].

• Target Antigen:

  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 Weight:

  558.86

• 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.Harvard Medical School LINCS LIBRARY|J Cell Sci. 2015 Sep 1;128(17):3317-29. |Biochemistry. 2017 Jun 13;56(23):2921-2927.|Biochemistry. 2018 Feb 27;57(8):1369-1379.|bioRxiv. 2023 Oct 6.|J Biol Chem. 2012 Mar 23;287(13):9742-52.|J Med Chem. 2019 May 9;62(9):4772-4778.|Oncotarget. 2020 Nov 3;11(44):3921-3932.|Sci Transl Med. 2018 Jul 18;10(450):eaaq1093.

• Shipping Conditions:

  Room Temperature

• Storage Conditions:

  4°C (Powder, sealed storage, away from moisture)

• Clinical Information:

  Phase 2

• CAS Number:

  289499-45-2