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Canertinib (dihydrochloride)

Product Specifications

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)

Product Datasheet

http://file.medchemexpress.com/batch_PDF/HY-10367A/Canertinib-dihydrochloride-DataSheet-MedChemExpress.pdf

Product MSDS

http://file.medchemexpress.com/batch_PDF/HY-10367A/Canertinib-dihydrochloride-SDS-MedChemExpress.pdf

Clinical Information

Phase 2

CAS Number

289499-45-2

Available Sizes

Curated Selection

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