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.
|Source||Biochem Biophys Res Commun (2015). Figure 3. Erlotinib Hydrochloride|
|Cell Lines||Female BALB/c nude mice|
|Incubation Time||24 h|
|Results||Erlotinib exerts its anti-tumor effect by inhibiting the intracellular phosphorylation of tyrosine kinase which is related to EGFR. We investigated whether the administration time can affect the ability of erlotinib to inhibit the phosphorylation of EGFR. Under non-drugged state, the phosphorylation of EGFR showed obvious oscillation (p < 0.05, Fig. 3A).|
|Source||Biochem Biophys Res Commun (2015). Figure 2. Erlotinib Hydrochloride|
|Cell Lines||Female BALB/c nude mice|
|Incubation Time||21 d|
|Results||Large areas of cystic degeneration and inflammatory infiltration can be easily spotted in the tumor tissue of mice given erlotinib at 08:00, 12:00 and 04:00, and the tumor cells arranged irregularly with necrosis and minimal bleeding.|
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.
|Related EGFR/HER2 Products|
Pertuzumab, a humanized monoclonal antibody and the first in the class of agents called the HER2 dimerization inhibitors, impairs the ability of HER2 to bind to other members of the HER family, MW: 148 KD.
Trastuzumab is a humanized, recombinant monoclonal antibody that binds to the extracellular domain of HER2, MW:145.53 KD.
Anlotinib is a EGFR inhibitor extracted from patent 2015185012 A1, compound 1，which can be used to treat non-small cell lung cancer.
Cetuximab, a novel molecular-targeted agent,is an inhibitor of EGFR monoclonal humanized antibody interacting with the extracellular binding site of EGFR to block ligand stimulation. MW : 145.781 KD.
EAI045 is an allosteric inhibitor that targets selected drug-resistant EGFR mutants but spares the wild-type receptor.
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2017 AbMole BioScience. All Rights Reserved.