Canertinib

• Description :

  Canertinib (CI-1033; PD-183805) is a potent and irreversible EGFR inhibitor; inhibits cellular EGFR and ErbB2 autophosphorylation with IC50s of 7.4 and 9 nM. Canertinib is active against vaccinia virus respiratory infection in mice[1][2][3][4].

• CAS Number :

  [267243-28-7]

• Product Name Alternative :

  CI-1033; PD-183805

• UNSPSC :

  12352005

• Hazard Statement :

  H302, 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.html

• Purity :

  99.74

• Solubility :

  DMSO : 4.9 mg/mL (warming) |Ethanol : 12.5 mg/mL (ultrasonic)

• Smiles :

  O=C(NC1=C(C=C2C(C(NC3=CC=C(C(Cl)=C3)F)=NC=N2)=C1)OCCCN4CCOCC4)C=C

• Molecular Formula :

  C24H25ClFN5O3

• Molecular Weight :

  485.94

• Precautions :

  H302, 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.

• Shipping Conditions :

  Room Temperature

• Storage Conditions :

  -20°C, 3 years; 4°C, 2 years (Powder)

• Scientific Category :

  Reference compound1

• Clinical Information :

  Phase 2

• Isoform :

  EGFR/ErbB1/HER1; ErbB2/HER2

• Citation 01 :

  Biochemistry. 2017 Jun 13;56 (23) :2921-2927.|Biochemistry. 2018 Feb 27;57 (8) :1369-1379.|bioRxiv. 2024 Jan 4:2023.10.06.561161.|Hepatol Int. 2025 Nov 3.|J Biol Chem. 2012 Mar 23;287 (13) :9742-52.|J Med Chem. 2019 May 9;62 (9) :4772-4778.|J Med Chem. 2025 Aug 28;68 (16) :17917-17932.|Oncotarget. 2020 Nov 3;11 (44) :3921-3932.|Sci Transl Med. 2018 Jul 18;10 (450) :eaaq1093.|Harvard Medical School LINCS LIBRARY|J Cell Sci. 2015 Sep 1;128 (17) :3317-29.