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ICONC13994 Pelitinib(EKB-569) (257933-82-7)
 
 
Catalog No.: C13994
CAS No.: 257933-82-7
Synonym: WAY-EKB-569,WAY-EKB 569,NSC729742,WAY-172569,D05399
Chemical Name:

(2E)-N-[4-[(3-Chloro-4-fluorophenyl)amino]-3-cyano-7-ethoxy-6-quinolinyl]-4-(dimethylamino)-2-butenamide

Molecular Formula: C24H23ClFN5O2
Molecular Weight: 467.92
 
Technical Data:
Appearance:
Solubility: Soluble in Ethanol
Purity: >99%
Storage: at -20℃ 2 years
Original QC Data:
Shipping Conditions: Ambient Temp.
 
Price and Availability of Pelitinib(EKB-569):

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Biological Activity:

A tyrosine kinase inhibitor that is used to prepare formulation for treating primary or secondary cancer.Pelitinib is a 3-cyanoquinoline pan-ErbB tyrosine kinase inhibitor with potential antineoplastic activity. EKB-569 irreversibly binds covalently to epidermal growth factor receptors (EGFR) ErbB-1, -2 and -4, thereby inhibiting receptor phosphorylation and signal transduction and resulting in apoptosis and suppression of proliferation in tumor cells that overexpress these receptors. EKB-569 inhibits EGF-induced phosphorylation of EGF-R and the growth of tumors that overexpress EGF-R in animal models.

 
References:
Hegedüs C  et al. 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 84:260-7 (2012).
 
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