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Pelitinib (EKB-569)EGFR inhibitor,potent and irreversible

Pelitinib (EKB-569)

Catalog No. A1835
Size Price Stock Qty
10mM (in 1mL DMSO) $105.00 In stock
5mg $85.00 In stock
25mg $300.00 In stock
100mg $800.00 In stock

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Sample solution is provided at 25 µL, 10mM.

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Chemical structure

Pelitinib (EKB-569)

Biological Activity

Description Pelitinib is a potent irreversible inhibitor of EGFR with IC50 value of 38.5 nM.
Targets EGFR          
IC50 38.5 nM          

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Chemical Properties

Cas No. 257933-82-7 SDF Download SDF
Chemical Name (E)-N-[4-(3-chloro-4-fluoroanilino)-3-cyano-7-ethoxyquinolin-6-yl]-4-(dimethylamino)but-2-enamide
Canonical SMILES CCOC1=C(C=C2C(=C1)N=CC(=C2NC3=CC(=C(C=C3)F)Cl)C#N)NC(=O)C=CCN(C)C
Formula C24H23ClFN5O2 M.Wt 467.92
Solubility >11.7mg/mL in DMSO Storage Store at -20°C
General tips N/A
Shipping Condition N/A

Background

Pelitinib (also known as EKB-569), a 3-cyanoquinoline, is a potent, and irreversible inhibitor of epidermal growth factor receptor (EGF-R) tyrosine kinase that inhibits the activity of EGF-R with the half maximal inhibition concentration IC50 value of 38.5 nM in vitro [1].

Pelitinib has been found to exert a potent anti-proliferative activity against tumor cells overexpressing EGF-R, including NHEK, A431 and MDA-468 cells, with IC50 values of 61 nM, 125 nM and 260 nM respectively; while it has also been found to potently inhibit EGF-induced phosphorylated EGF-R (pEGF-R) in A431 and NHEK cells with IC50 values ranging from 20 nM to 80 nM [2].

References:
[1] Torrance CJ, Jackson PE, Montgomery E, Kinzler KW, Vogelstein B, Wissner A, Nunes M, Frost P, Discafani CM. Combinatorial chemoprevention of intestinal neoplasia. Nat Med. 2000 Sep;6(9):1024-8.
[2] Nunes M, Shi C, Greenberger LM. 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 Jan;3(1):21-7.