Pelitinib
Tocris Bioscience, part of Bio-Techne | Catalog # 6349
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
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 IncProduct Specifications
Molecular Weight
467.92
Formula
C24H23ClFN5O2
Storage
Store at -20°C
Purity
≥97% (HPLC)
Chemical Name
(2E)-N-[4-[(3-Chloro-4-fluorophenyl)amino]-3-cyano-7-ethoxy-6-quinolinyl]-4-(dimethylamino)-2-butenamide
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.
Solubility
| 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 all 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 |
Calculators
Molarity Calculator
Dilution Calculator
Reconstitution Calculator
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 Specific Notices for Pelitinib
For research use only
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