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.

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.
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HPLC-MS/MS 测定大鼠血浆中新型 B-Raf(V600E) 和 EGFR 双重抑制剂及其在药代动力学研究中的应用。

DOI:
10.1016/j.jpba.2016.06.049
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发表时间:
2016
影响因子:
3.4
通讯作者:
Hui
Hui
中科院分区:
医学3区
文献类型:
--
作者:
Zhi;Jifeng Deng;Ying;Yu Chang;Hui

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EGFR和B-RafV 600 E双重抑制是治疗B-RafV 600 E突变的结直肠癌患者的一种有前途的策略。先前,化合物3被设计和合成为新型B-RafV 600 E和EGFR双重抑制剂,其在基于激酶和细胞的测定中具有高度效力。本文建立了一种灵敏、快速的HPLC-MS/MS定量方法,并验证了该方法的有效性,可用于进一步评价化合物3在大鼠体内的药代动力学。
The EGFR and B-RafV600Edual inhibition is a promising strategy in treatment of colorectal cancer patients with B-RafV600Emutation. Previously, compound 3 was designed and synthesized as a novel B-RafV600Eand 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.
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