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Potent irreversible EGFR inhibitor (IC50 = 20-80 nM). Selective for EGFR over Src, MEK/ERK, erbB2, Raf, c-Met and Cdk4 (IC50 values are 282, 800, 1255, 3353, 4100 and >20,000). Inhibits the growth of tumors overexpressing EGFR in vivo. Orally bioavailable.
Sold for research purposes under agreement from Pfizer Inc
|Storage||Store at -20°C|
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.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 467.92. 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|
|0.5 mM||4.27 mL||21.37 mL||42.74 mL|
|2.5 mM||0.85 mL||4.27 mL||8.55 mL|
|5 mM||0.43 mL||2.14 mL||4.27 mL|
|25 mM||0.09 mL||0.43 mL||0.85 mL|
References are publications that support the biological activity of the product.
Nunes et al (2004) Phosphorylation of extracellular signal-regulated kinase 1 and 2, protein kinase B, and signal transducer and activator of transcription 3 are differently inhibited by an epidermal growth factor receptor inhibitor, EKB-569, in tumor cells and normal human Mol.Cancer Ther. 3 21 PMID: 14749472
Hegedüs (2012) Interaction of the EGFR inhibitors gefitinib, vandetanib, pelitinib and neratinib with the ABCG2 multidrug transporter: Implications for the emergence and reversal of cancer drug resistance Biochem. Pharmacol. 84 260 PMID: 22548830
Tyner et al (2006) Blocking airway mucous cell metaplasia by inhibiting EGFR antiapoptosis and IL-13 transdifferentiation signals. J.Clin.Invest. 116 309 PMID: 16453019
Torrance et al (2000) Combinatorial chemoprevention of intestinal neoplasia. Nat.Med. 6 1024 PMID: 10973323
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Keywords: Pelitinib, Pelitinib supplier, EKB-569, orally, active, potent, irreversible, EGFR, inhibitors, inhibits, ErbB-1, in, vivo, 6349, Tocris Bioscience
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Literature in this Area
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Schizophrenia is a debilitating psychiatric disorder that affects 1% of the worldwide population. This poster describes the neurobiology of Schizophrenia, as well as highlighting the genetic and environmental factors that play a fundamental role in the etiology of the disease. The current and emerging drug targets are also discussed.