Erlotinib Hydrochloride also known as Tarceva, CP-358774, OSI-774 and NSC-718781, is an inhibitor of human EGFR tyrosine kinase (IC50 = 2 nM) and decreases EGFR autophosphorylation in tumor cells (IC50 = 20 nM). Erlotinib specifically targets the epidermal growth factor receptor (EGFR) tyrosine kinase, which is highly expressed and occasionally mutated in various forms of cancer. It binds in a reversible fashion to the adenosine triphosphate (ATP) binding site of the receptor.
|Cell lines||BxPC-3 and MIAPaCa cells|
|Preparation method||Cell Viability Assay To test the viability of cells treated with B-DIM, erlotinib, or the combination, BxPC-3 and MIAPaCa cells were plated (3,000-5,000 per well) in a 96-well plate and incubated overnight at 37jC. We initially tested a range of concentrations for both B-DIM (10-50 µmol/L) and erlotinib (1-5 µmol/L). Based on the initial results, the concentration of B-DIM (20 Amol/L) and erlotinib (2 Amol/L) were chosen for all assays. The effects of B-DIM (20 µmol/L), erlotinib (2 µmol/L), and the combination on BxPC-3 and MIAPaCa cells were determined by the standard 3-(4,5- dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay after 72 h and was repeated three times. The color intensity was measured by a Tecan microplate fluorometer at 595 nm. DMSO-treated cells were considered to be the untreated control and assigned a value of 100%.|
|Incubation time||72 h|
|Animal models||SCID mice bearing orthotopically implanted BxPC-3 pancreatic tumor cells|
|Dosages||50 mg/kg body weight every day for 15 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.
Schedule-dependent cytotoxic synergism of pemetrexed and erlotinib in BXPC-3 and PANC-1 human pancreatic cancer cells.
Wang et al. Exp Ther Med. 2011 Sep;2(5):969-975. PMID: 22977607.
Molecular mechanisms and modulation of key pathways underlying the synergistic interaction of sorafenib with erlotinib in non-small-cell-lung cancer (NSCLC) cells.
Giovannetti et al. Curr Pharm Des. 2012 Sep 7. PMID: 22973961.
Clinical and economic review of erlotinib in non-small-cell lung cancer.
Yeung et al. Expert Rev Pharmacoecon Outcomes Res. 2012 Aug;12(4):411-23. PMID: 22971028.
Erlotinib has better efficacy than gefitinib in adenocarcinoma patients without EGFR-activating mutations, but similar efficacy in patients with EGFR-activating mutations.
Wu et al. Exp Ther Med. 2012 Feb;3(2):207-213. PMID: 22969870.
Temporal molecular and biological assessment of an erlotinib-resistant lung adenocarcinoma model reveals markers of tumor progression and treatment response.
Weaver et al. Cancer Res. 2012 Sep 11. PMID: 22969147.
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