Canertinib dihydrochloride

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Description: Potent EGFR kinase inhibitor
Alternative Names: CI 1033,PD 183805
Chemical Name: N-[4-[(3-Chloro-4-fluorophenyl)amino]-7-[3-(4-morpholinyl)propoxy]-6-quinazolinyl]-2-propenamide dihydrochloride
Purity: ≥98% (HPLC)
Literature (1)

Biological Activity for Canertinib dihydrochloride

Canertinib dihydrochloride is a potent EGFR kinase inhibitor (IC50 = 7.4 nM). Blocks autophosphorylation of erbB2. Inhibits growth of A431 tumor xenografts in mice. Cell permeable.

Licensing Information

Sold for research purposes under agreement from Pfizer Inc.

Technical Data for Canertinib dihydrochloride

M. Wt 558.86
Formula C24H25ClFN5O3.2HCl
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 289499-45-2
PubChem ID 156413
Smiles O=C(C=C)NC1=C(OCCCN4CCOCC4)C=C(N=CN=C2NC3=CC(Cl)=C(F)C=C3)C2=C1.Cl.Cl

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data for Canertinib dihydrochloride

Solvent Max Conc. mg/mL Max Conc. mM
water 11.18 20
DMSO 55.89 100

Preparing Stock Solutions for Canertinib dihydrochloride

The following data is based on the product molecular weight 558.86. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.79 mL 8.95 mL 17.89 mL
5 mM 0.36 mL 1.79 mL 3.58 mL
10 mM 0.18 mL 0.89 mL 1.79 mL
50 mM 0.04 mL 0.18 mL 0.36 mL

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Product Datasheets for Canertinib dihydrochloride

References for Canertinib dihydrochloride

References are publications that support the biological activity of the product.

Smaill et al (2000) 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. 43 1380 PMID: 10753475

If you know of a relevant reference for Canertinib dihydrochloride, please let us know.

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Citations for Canertinib dihydrochloride

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Literature in this Area

Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!

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