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Pelitinib

Cat. No. M1904
Pelitinib Structure
Synonym:

EKB-569

Size Price Availability Quantity
10mg USD 160 In stock
50mg USD 580 In stock
100mg USD 1020 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

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.

Protocol
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.
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
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.

Chemical Information
Molecular Weight 467.92
Formula C24H23ClFN5O2
CAS Number 257933-82-7
Purity >99%
Solubility DMSO 10 mg/mL
Storage at -20°C
References

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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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: Pelitinib, EKB-569 supplier, EGFR/HER2, inhibitors

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