Erlotinib is an EGFR inhibitor with IC50 of 2 nM, >1000-fold more sensitive for EGFR than human c-Src or v-Abl.
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
|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.|
|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 Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 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 Compound A of 10 mg/kg.
|Solubility||65 mg/mL in DMSO|
 Wu YL, et al. Ann Oncol. 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.
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