商品编号


EL-014-NP



品牌


Signosis



公司


Signosis



公司分类


Cell-Based Assays




1 Ea

商品信息

Description:
Epidermal growth factor receptor (EGFR) is a cell-surface receptor with intrinsic intracellular protein-tyrosine kinase (TK) activity. Ligand binding induces EGFR dimerization and phosphorylation, le
ADI
ng to the activation of EGFR signaling pathway. In several malignancies such as non-small cell lung cancer (NSCLC), EGFR signaling is deregulated due to mutations in EGFR, which results in uncontrolled proliferation and migration of tumor cells. EGFR mutations can lead to “oncogene-addicted” cancers, where the tumor cells depend on the mutated EGFR for cell survival and malignant phenotype. ?One of the most common EGFR mutations found in human patients is L858R substitution in exon 21, within the activation loop of EGFR. Patients with this mutation are sensitive to EGFR tyrosine kinase inhibitors (TKIs) such as gefitinib or erlotinib, whereas patients with wild type EGFR are not sensitive to TKI. Another clinically relevant mutation associated with acquired gefitinib and erlotinib resistance is T790M, found in exon 20. Cells expressing EGFR with both L858R and T790M mutations are resistant to induced apoptosis in the presence of gefitinib or erlotinib.?
Data:
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Dose-dependent growth inhibition of BaF3 cells harboring EGFR Del19 (EL-011), EGFR Ins19 (EL-009) and representative Erlotinib resistant cell line, EGFR Del19-T790M (EL-014). The cells were treated with the indicated dose of erlotinib for 24 hours and cells vi
ABI
lity was measured using
Signosis
CVC reagent. EGFR Del19 stably expressing BaF3 cells (EL-011) remains 14-fold more sensitive to TKI erlotinib (IC50=0.34) than its resistance derivative EGFR Del19-T790M stably expressing BaF3 cells (EL-014) (IC50=4.9).

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