Pelitinib

Name: Pelitinib
Brand: Tocris Bioscience
SKU: 6349

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

Citations (1)

COA / SDS

Potent and irreversible EGFR inhibitor; orally bioavailable

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.

Solubility for Pelitinib

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
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

Molarity Calculator

Calculate the mass, volume, or concentration required for a solution.

Mass

Concentration

Volume

M. Wt*

g/mol

*When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and CoA (available online).

Dilution Calculator

Calculate the dilution required to prepare a stock solution.

Concentration 1 (C1)

Volume 1 (V1)

Concentration 2 (C2)

Volume 2 (V2)

Reconstitution Calculator

The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial. Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.

Volume (to add to vial)

Mass (in vial)

Desired Reconstitution Concentration

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