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Submit ReviewCanertinib dihydrochloride
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)
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 |
| InChI Key | JZZFDCXSFTVOJY-UHFFFAOYSA-N |
| 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 | |
|---|---|---|---|
| Solubility | |||
| 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.
| 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
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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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Cancer Research Product Guide
A collection of over 750 products for cancer research, the guide includes research tools for the study of:
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A collection of over 400 products for kinase research, the listing includes inhibitors of:
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