Biological Activity
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
| 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.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 55.89 | 100 | |
| water | 11.18 | 20 |
Preparing Stock Solutions
The following data is based on the product molecular weight 558.86. Batch specific molecular weights may vary from batch to batch due to solvent 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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References
References are publications that support the products' biological activity.
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
Keywords: Canertinib dihydrochloride, supplier, potent, EGFR, receptor, tyrosine, kinase, epidermal, growth, factor, RTK, anticancer, inhibitors, inhibits, PD183805, CI1033, CI, 1033, PD, 183805, EGFR, EGFR, Tocris Bioscience
