Erlotinib is an EGFR inhibitor with IC50 of 2 nM, >1000-fold more sensitive for EGFR than human c-Src or v-Abl.
|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.
|Solubility||78 mg/mL in DMSO|
|Source||Sci Rep (2017). Figure 1. Erlotinib (AbMole Bioscience, Houston, TX)|
|Method||bacterial cell wall-induced lipolysis|
|Cell Lines||Murine 3T3-L1 preadipocytes|
|Incubation Time||48 h|
|Results||FK565-stimulated glycerol release was lower in 3T3-L1 adipocytes pre-incubated with TKIs ponatinib, dasatinib, dafabranib, vandetanib, ruxolitinib, SB203580, ibrutinib, gefitinib, sorafenib, neratinib, erlotinib, at 1–10 μM.|
Sci Rep. 2017 May 8;7(1):1578.
Tyrosine kinase inhibitors of Ripk2 attenuate bacterial cell wallmediated lipolysis, inflammation and dysglycemia
Erlotinib purchased from AbMole
First-line erlotinib versus gemcitabine/cisplatin in patients with advanced EGFR mutation-positive non-small-cell lung cancer: analyses from the phase III, randomized, open-label, ENSURE study.
Wu YL, et al. Ann Oncol. 2015 Sep;26(9):1883-9. PMID: 26105600.
|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.
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