Potent epidermal growth factor receptor (EGFR) kinase inhibitor (IC50 = 0.7 μM) that displays 50-fold and >140-fold selectivity over ErbB2 and insulin receptor kinase respectively. Induce G1 growth arrest selectively in transformed cells (IC50 values are 6.4 and 9.4 μM in HPV16-immortalized and normal keratinocytes respectively).
|Storage||Desiccate at +4°C|
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.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 322.36. 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||3.1 mL||15.51 mL||31.02 mL|
|5 mM||0.62 mL||3.1 mL||6.2 mL|
|10 mM||0.31 mL||1.55 mL||3.1 mL|
|50 mM||0.06 mL||0.31 mL||0.62 mL|
References are publications that support the products' biological activity.
Ben-Bassat et al (1999) Tyrphostins that suppress the growth of human papilloma virus 16-immortalized human keratinocytes. J.Pharmacol.Exp.Ther. 290 1442 PMID: 10454524
Gazit et al (1991) Tyrphostins. 2. Heterocyclic and α-substituted benzylidenemalononitrile tyrophostins as potent inhibitors of EGF receptor and ErbB2/neu tyrosine kinases. J.Med.Chem. 34 1896 PMID: 1676428
Levitzki and Gazit (1995) Tyrosine kinase inhibition: an approach to drug development. Science 267 1782 PMID: 7892601
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