Gefitinib (ZD-1839, Iressa) is a novel potent EGFR tyrosine kinase inhibitor with an IC50 of 0.40nM.Gefitinib (ZD-1839,Iressa) selectively inhibited EGF-stimulated growth of HUVECs (IC50 = 0.03 - 0.1 µM) compared with FGF- or VEGF-stimulated growth (IC50 = 1 - 3 µM for both).Gefitinib is a competitive inhibitor with respect to ATP (Ki = 2.1 nM) when the peptide substrate concentration was fixed at 2 mM (6-fold higher than the Km) and the ATP concentration was varied. Gefitinib showed noncompetitive kinetics (Ki = 15.0 nM) when the ATP concentration was 50 µM (6-fold higher than the Km) and the peptide concentration was varied.
|Source||Clin Cancer Res (2017). Figure 2. Gefitinib (Abmole Bioscience)|
|Cell Lines||HCC4006 and H1975 cells|
|Incubation Time||72 h|
|Results||We found directly inducing EMT by exogenous TWIST activation (Fig. 2) or chronic TGF- β treatment (Sup. Fig. 2) led to depressed levels of BIM resulting in suppression of EGFRi-induced apoptosis and resistance to EGFRi (WZ4002 and gefitinib).|
|Cell lines||MDA-361, SKBR-3, MDA-453 and BT-474 cells|
|Preparation method||Monolayer Growth and Anchorage-independent Growth Assays. For monolayer growth, cells were seeded at a density of 3–4 104 cells in 12-well plates. Twenty-four h later, ZD1839 was added to the cells. Fresh medium ZD1839 was replaced on day 3. On day 5, cells were harvested by trypsinization and counted with a Zeiss Coulter Counter (Beckman Coulter, Miami, FL). Colony-forming assays in soft agarose were performed as described previously (30). Tumor cell colonies measuring 50 m were counted after 7 days using an Omnicon 3800 colony counter and Tumor Colony Analysis V2.IIA software (Imaging Products International, Inc.).|
|Concentrations||0.1–10 µ M|
|Incubation time||4 days|
|Animal models||BT-474 cells Xenograft in Athymic Mice|
|Formulation||0.05% Tween 80|
|Dosages||200 mg/kg/day for 28 days|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
Method development and validation for the quantification of dasatinib, erlotinib, gefitinib, imatinib, lapatinib, nilotinib, sorafenib and sunitinib in human plasma by liquid chromatography coupled with tandem mass spectrometry.
Lankheet NA et al. Biomed Chromatogr. 2012 Sep 17. PMID: 22987603.
A pilot study for the early assessment of the effects of BMS-754807 plus gefitinib in an H292 tumor model by [(18)F]fluorothymidine-positron emission tomography.
Lee SJ et al. Invest New Drugs. 2012 Sep 18. PMID: 22987020.
Gefitinib-Induced Paronychia: Response to Autologous Platelet-Rich Plasma.
Kwon SH et al. Arch Dermatol. 2012 Sep 17;1-4. PMID: 22986691.
Polymorphisms to predict outcome to the tyrosine kinase inhibitors gefitinib, erlotinib, sorafenib and sunitinib.
Erdem L et al. Curr Top Med Chem. 2012 Sep 11. PMID: 22978339.
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