Pelitinib

Name: Pelitinib
Brand: Tocris Bioscience
SKU: 6349

Tocris Bioscience, part of Bio-Techne | Catalog # 6349

Citations (2)

COA / SDS

Potent and irreversible EGFR inhibitor; orally bioavailable

Discontinued Product

6349 has been discontinued. View all EGF Receptor Inhibitors products.

Key Product Details

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)
Molecular Weight:	467.92

View Full Technical Details for Pelitinib

Technical Data
Citations

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.

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References for Pelitinib

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