Pelitinib

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Cat.No. 6349 - Pelitinib | C24H23ClFN5O2 | CAS No. 257933-82-7
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)
Datasheet
Citations
Reviews
Literature

Biological Activity

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

Technical Data

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

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 23.4 50

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 solvent 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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References

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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Literature in this Area

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