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Figure 6 | Molecular Cancer

Figure 6

From: Metabolism of the EGFR tyrosin kinase inhibitor gefitinib by cytochrome P450 1A1 enzyme in EGFR-wild type non small cell lung cancer cell lines

Figure 6

Conditions affecting gefitinib metabolism: hypoxia, cigarette smoke extract and cell density. A) H322 cells were incubated with 0.1 μM [3H]gefitinib under normoxia or hypoxia for the indicated times. Values given of gefitinib content, expressed as pmol/mg of protein, are the means (± SD) of four independent determinations (**P < 0.01; ***P < 0.001). B) Calu-3 cells were treated for 24 h with 2.5% of CSE and then exposed to 0.1 μM [3H]gefitinib for the indicated times. Values given are the means (± SD) of three independent determinations (**P < 0.01; ***P < 0.001). Inset: EROD assay performed in cells untreated or treated for 24 h with 1, 2.5 or 5% CSE expressed as pmol Res/mg protein/min. C) Calu-3 cells were seeded at different cell density (from 7000 to 70000 cells/cm2) and after 24 h incubated for 0.5 h () or 24 h (■) with 0.1 μM [3H]gefitinib. Then, the intracellular [3H]gefitinib content was determined and plotted versus final cell density expressed as μg protein/cm2. Inset: values are expressed as % of reduction versus 0.5 h value. D) Calu-3 seeded at low and high density (7000 and 70000 cells/cm2 respectively)were exposed for 72 h to different concentrations of gefitinib. Cell growth was assessed using crystal violet staining. Data are expressed as percent inhibition of cell proliferation versus control cells. The mean values of three independent measurements (± SD) are shown (*P < 0.05; ***P < 0.001).

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