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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 Experiment | |
|---|---|
| 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 Experiment | |
|---|---|
| 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 |
| Administration | PO. |
| Molecular Weight | 467.92 |
| Formula | C24H23ClFN5O2 |
| CAS Number | 257933-82-7 |
| Solubility (25°C) | DMSO 10 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
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| Sapitinib (AZD8931)
AZD8931 (Sapitinib) is an equipotent, reversible inhibitor of Signaling by EGFR, ERBB2 (HER2), and ERBB3 with IC50 of 4, 3, 4 nM respectively. |
| Afatinib
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| Erlotinib Hydrochloride
Erlotinib is an inhibitor of human EGFR tyrosine kinase (IC50 = 2 nM) and decreases EGFR autophosphorylation in tumor cells (IC50 = 20 nM). |
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