Biological Activity
High affinity and potent covalent EGFR kinase inhibitor (Ki = 0.14 nM). Inhibits autophosphorylation of WT and mutant EGFR in tumor cells (IC50 values are 5.8 and 6.6 nM, respectively).
Licensing Information
Sold for research purposes under agreement from Pfizer Inc.
Technical Data
| M. Wt | 372.78 |
| Formula | C18H14ClFN4O2 |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 1035638-91-5 |
| PubChem ID | 74766099 |
| InChI Key | TUYDDIWQXWTNSW-UHFFFAOYSA-N |
| Smiles | COC1=CC2=C(C(NC3=CC(Cl)=C(C=C3)F)=NC=N2)C=C1NC(C=C)=O |
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 | 37.28 | 100 | |
| ethanol | 3.73 | 10mM with gentle warming |
Preparing Stock Solutions
The following data is based on the product molecular weight 372.78. 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 | 2.68 mL | 13.41 mL | 26.83 mL |
| 5 mM | 0.54 mL | 2.68 mL | 5.37 mL |
| 10 mM | 0.27 mL | 1.34 mL | 2.68 mL |
| 50 mM | 0.05 mL | 0.27 mL | 0.54 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Schwartz et al (2014) Covalent EGFR inhibitor analysis reveals importance of reversible interactions to potency and mechanisms of drug resistance. Proc.Natl.Acad.Sci.U.S.A. 111 173 PMID: 24347635
Keywords: PF 6274484, supplier, PF6274484, epidermal, growth, factor, receptors, EGFR, kinase, inhibitors, inhibits, potent, high, affinity, covalent, EGFR, EGFR, Tocris Bioscience
