Pelitinib

Key Product Details

Product Description

Pelitinib is a 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.

Licensing Information

Sold for research purposes under agreement from Pfizer Inc

Product Specifications for Pelitinib

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Solubility

Preparing Stock Solutions for Pelitinib

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 all affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:

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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

Calculators

Background References

References are publications that support the biological activity of the product.

• Torrance Combinatorial chemoprevention of intestinal neoplasia. Nat.Med. 2000 PMID: 10973323
• Hegedüs 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. 2012 PMID: 22548830
• Tyner Blocking airway mucous cell metaplasia by inhibiting EGFR antiapoptosis and IL-13 transdifferentiation signals. J.Clin.Invest. 2006 PMID: 16453019
• Nunes 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. 2004 PMID: 14749472

Product Documents for Pelitinib