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United States (Change Country)Gefitinib (Iressa) Chemical Structure
Gefitinib (Iressa) is a novel potent EGFR tyrosine kinase and Akt phosphorylations inhibitor with IC50 of 37, 26 and 57 nM for Tyr1173, Tyr1173 and Tyr992 in, respectively, the low and high EGFR expressing cell lines. Immunoblot analysis of whole cell lysates revealed that in general gefitinib effectively inhibited all tyrosine phosphorylation sites on EGFR in both the high and low-EGFR-expressing cell lines. However, the phosphorylation sites Tyr1173 and Tyr992 were less sensitive requiring higher concentrations of gefitinib for inhibition. As was the case for ERK, gefitinib fails to effectively inhibit AKT phosphorylation in the high-EGFR-
expressing cell line indicating that EGFR is not the major activator of AKT in this cell line. The low IC50 (7 nM), however show that the weak induction of AKT phosphorylation by EGFR in this cell line is efficiently blocked by gefitinib. Gefitinib inhibits AKT phosphorylations, with IC50 values of 220 and 263 nM, in the low-EGFR- and –EGFRvIII-expressing cell lines, respectively. [1] MCF10A cells are nontransformed breast epithelial cells that require EGF to proliferate. The monolayer growth of these EGF-driven untransformed cells is inhibited by ZD1839 with an IC50 of 20 nM, similar to its IC50 in vitro for EGFR and consistent with effective inhibition of EGFR in vivo. [2] Cell line characteristics and sensitivity to ZD1839 at 1uM are 59% inhibition for MDA-MB-231,74% inhibition for A431, 81% inhibition for SKBr3,60% inhibition for SKOV3, 33% inhibition for BT474,52% inhibition for MCF-7, 28% inhibition for T47D, respectively. [3]
[1] CANCER RESEARCH October 1, 2001;7184–7188
[2] Int. J. Cancer. 2001;774–782
| Molecular Weight (WM): | 446.90 |
|---|---|
| Formula: | C22H24ClFN4O3 |
| Solubility(R.T.:25°C): | DMSO 89mg/mL |
| Water <1mg/mL | |
| Ethanol 4mg/mL |
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;Mol Biosyst, 2011, 7(12), 3223-33 Gefitinib (Iressa) purchased from Selleck
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Data from [Carcinogenesis 2010;31, 1948–1955] Gefitinib (Iressa) purchased from Selleck
;Dr Zhang of Tianjin Medical University Gefitinib (Iressa) purchased from Selleck
;Dr Vicky Tin from University of Hong Kong Gefitinib (Iressa) purchased from Selleck
Data from [Mol Syst Biol 2011;7, 486] Gefitinib (Iressa) purchased from Selleck
Data from [Oncogene 2010;30, 737-750] Gefitinib (Iressa) purchased from Selleck
Data from [Antiviral Res 2010;89, 64-70] Gefitinib (Iressa) purchased from Selleck
Data from [Carcinogenesis 2010;31, 1948–1955] Gefitinib (Iressa) purchased from Selleck
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