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Submit ReviewPelitinib
Description: Potent and irreversible EGFR inhibitor; orally bioavailable
Alternative Names: EKB-569
Chemical Name: (2E)-N-[4-[(3-Chloro-4-fluorophenyl)amino]-3-cyano-7-ethoxy-6-quinolinyl]-4-(dimethylamino)-2-butenamide
Purity: ≥97% (HPLC)
Biological Activity for Pelitinib
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
Compound Libraries for Pelitinib
Pelitinib is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.
Technical Data for Pelitinib
| M. Wt | 467.92 |
| Formula | C24H23ClFN5O2 |
| Storage | Store at -20°C |
| Purity | ≥97% (HPLC) |
| CAS Number | 257933-82-7 |
| PubChem ID | 6445562 |
| InChI Key | WVUNYSQLFKLYNI-AATRIKPKSA-N |
| Smiles | O=C(/C=C/CN(C)C)NC1=C(OCC)C=C(N=CC(C#N)=C2NC3=CC=C(F)C(Cl)=C3)C2=C1 |
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.
Solubility Data for Pelitinib
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 23.4 | 50 |
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 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 |
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Product Datasheets for Pelitinib
References for Pelitinib
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
If you know of a relevant reference for Pelitinib, please let us know.
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Citations for Pelitinib
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Literature in this Area
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Angiogenesis in Cancer Poster
This poster summarizes the pathogenesis of angiogenesis in cancer, as well as some of the main angiogenesis therapeutic targets.