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Product Details
Synonyms EKB-569
Product Type Chemical
Formula C24H23ClFN5O2
MW 467.9
CAS 257933-82-7
Purity Chemicals ≥95%
Appearance Solid.
Solubility Soluble in DMSO or ethanol.
Declaration Manufactured by SynKinase.
Other Product Data Target: EGFR - HER2 | Kinase Group: RTK | Substrate: Tyrosine

Click here for Original Manufacturer Product Datasheet
Our product description may differ slightly from the original manufacturers product datasheet.
Shipping and Handling
Shipping AMBIENT
Short Term Storage +4°C
Long Term Storage -20°C
Use/Stability Stable for at least 2 years after receipt when stored at -20°C.
MSDS Download PDF
Product Specification Sheet
Datasheet Download PDF
Pelitinib, also known as EKB 569, is a potent, irreversible inhibitor of the EGFR tyrosine kinase. Cell based IC(50) values range from 39nM to 80nM and in vitro kinase assays are in sub-nanomolar range for EGFR receptors. In xenograft tumor models using overexpressing A431 cells Pelitinib inhibits growth of tumors with effective doses of 3.5-10mg/kg/dl. Recent research also shows that Pelitinib can potentiate radiation induced killing of squamouse cell carcinoma via the inhibition of IR-induced NF-κB mediated cell survial pathway.
Product References
  1. Dual irreversible kinase inhibitors: quinazoline-based inhibitors incorporating two independent reactive centers with each targeting different cysteine residues in the kinase domains of EGFR and VEGFR-2: A. Wissner, et al.; Bioorg. Med. Chem. 15, 3635 (2007)
  2. A quantitative analysis of kinase inhibitor selectivity: M.W. Karaman, et al.; Nat. Biotechnol. 26, 127 (2008)
  3. Development of a new epidermal growth factor receptor positron emission tomography imaging agent based on the 3-cyanoquinoline core: synthesis and biological evaluation: F. Pisaneschi, et al.; Bioorg. Med. Chem. 18, 6634 (2010)
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