Pelitinib (EKB-569) is a novel Epidermal growth factor receptor (EGFR) inhibitor which has shown potential therapeutic efficiency in solid tumors. Pelitinib selectively inhibits EGFR signaling in airway epithelial cells in vivo. Pelitinib (EKB-569) significantly enhanced IR-induced cell death and apoptosis. Pelitinib (EKB-569) has shown high arrest and decreased the phosphorylation of AKT and ERK at the protein level. More importantly, Pelitinib (EKB-569) had higher efficacy in hepatocellular carcinoma (HCC), compared to first generation, reversible EGFR-TK inhibitors.
|Cell lines||A431, SKBR3 and SW620 cells line|
|Preparation method||Cell Proliferation Assay.
Three human carcinoma cell lines, A431 (epidermoid carcinoma), SKBR3 (breast carcinoma), and SW620 (colon carcinoma), were used for the cell proliferation assays. All cell lines were obtained from the American Type Culture Collection. Cells were maintained in RPMI-1640 medium supplemented with 5% fetal bovine serum. Cells were plated in 96-well plates at the densities of 5.0 × 104/mL. On the next day, compounds were dosed at 0.5, 5, 50, 500, and 5000 ng/mL concentrations and the cells were cultured for 2 days. At the end of incubation, cell survival was determined by the sulforhodamine B assay as previously described.25 The IC50 values were obtained from the growth curves.
|Concentrations||0.5, 5, 50, 500 and 5000 ng/ml|
|Incubation time||2 days|
|Animal models||human epidermoid carcinoma A431 tumour xenograft model in Athymic nu/nu female mice|
|Formulation||0.2% Klucel or with 0.2% Klucel|
|Dosages||40 mg/kg for 28 consecutive 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.
|Solubility||DMSO 10 mg/mL|
Novel EGFR-TK inhibitor EKB-569 inhibits hepatocellular carcinoma cell proliferation by AKT and MAPK pathways.
Kim H, et al. J Korean Med Sci. 2011 Dec;26(12):1563-8. PMID: 22147992.
The PI3 kinase/mTOR blocker NVP-BEZ235 overrides resistance against irreversible ErbB inhibitors in breast cancer cells.
Brünner-Kubath C, et al. Breast Cancer Res Treat. 2011 Sep;129(2):387-400. PMID: 21046231.
Synthesis and structure-activity relationships of 6,7-disubstituted 4-anilinoquinoline-3-carbonitriles. The design of an orally active, irreversible inhibitor of the tyrosine kinase activity of the epidermal growth factor receptor (EGFR) and the human epidermal growth factor receptor-2 (HER-2).
Wissner A, et al. J Med Chem. 2003 Jan 2;46(1):49-63. PMID: 12502359.
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