Determination of a novel B-Raf(V600E) and EGFR dual inhibitor in rat plasma by HPLC-MS/MS and its application in a pharmacokinetic study

摘要

The EGFR and B-Raf(V600E) dual inhibition is a promising strategy in treatment of colorectal cancer patients with B-Raf(V600E) mutation. Previously, compound 3 was designed and synthesized as a novel B-Raf(V600E) and EGFR dual inhibitor with highly potency in both kinase and cell based assay. Herein, a sensitive and rapid HPLC-MS/MS quantitative method was developed and validated for the further pharmacokinetic evaluation of compound 3 in rats. (C) 2016 Elsevier B.V. All rights reserved.