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Pelitinib  -  EKB 569

CAS 257933-82-7

C24H23ClFN5O2  MW 467.92 

Purity: 99%

Soluble in DMSO to 77 mM 

Ordering Information:

Cat. No. Axon 1665    Prime Source

Qty1: 5 mg (research sample) / €125  $163

Qty2: 25 mg (research sample) / €450  $586

Qty3: on request contract research synthesis

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Biological Activity:   An irreversible inhibitor of EGFR tyrosine kinase with potential antineoplastic activity. Pelitinib irreversibly binds covalently to 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.   References: online   M Nunes et al. 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 keratinocytes. Mol. Cancer Ther. 2004, 3,21. [online]   C Erlichman et al. Phase I study of EKB-569, an irreversible inhibitor of the epidermal growth factor receptor, in patients with advanced solid tumors. J. Clin. Oncol. 2006, 24(15), 2252-2260. [online]   A Ocaña and E Amir. Irreversible pan-ErbB tyrosine kinase inhibitors and breast cancer: current status and future directions. Cancer Treat Rev. 2009, 5(8), 685-691. [online]     Chemical Name: (2E)-N-(4-((3-Chloro-4-fluorophenyl)amino)-3-cyano-7-ethoxyquinolin-6-yl)-4-(dimethylamino)but-2-enamide

Pelitinib | EGFR inhibitor | Axon Medchem | Axon 1665 | EKB 569 - WAY-EKB569

Axon Ligands ^TM - Research chemicals for biological study. Some high-profile samples could be provided under terms of contract research synthesis.

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