Gefitinib

Name Gefitinib
Supplier Cell Signaling Technology
Catalog 4765
Prices $129.00
Sizes 10 mg
Formula C22H24ClFN4O3
Molecular Weight 446.90 g/mol
Purity >99%
Description Gefitinib is a novel and potent EGFR tyrosine kinase inhibitor that binds to the ATP-binding site of the enzyme, and has been shown to be competitive with ATP and noncompetitive with peptide substrates (1). Gefitinib inhibits in vitro EGFR activity (IC 50 = 33 nM), significantly inhibits EGF-stimulated tumor cell growth (IC 50 = 54 nM) when compared to the absence of EGF (IC 50 = 8.8 µM), and effectively blocks EGF-stimulated autophosphorylation in tumor cells. It also selectively inhibits EGF-stimulated growth of HUVE cells compared with FGF- or VEGF-stimulated growth (1). Although studies demonstrate gefitinib to be much more selective for EGFR than HER2 (1,2), it has also shown to inhibit growth and phosphorylation of HER2 in numerous HER2-overexpressing cell lines (3).
Supplier Page Shop

Product images