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設計合成一係列用於治療胃癌的多靶點受體酪氨酸激酶抑製劑,並進行生物學評價。其中藥代動力學分析通過hjc黄金城進行

2023-07-06
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Gastric cancer is the second most lethal cancer across the world. Compounds 8f, inhibits FGFR1 signaling pathways as well as induces cell apoptosis, is a potential agent for the treatment of gastric cancer. The pharmacokinetical profile (PK) of 8f was tested in SD rats. Compound 8f showed an acceptable half-time of 3 h and displayed moderate maximum concentrations, which is enough to meet the concentration of the compound 8f to exert its efficacy in vivo. The pharmacokinetic analysis was performed by the testing service provided by Medicilon. 

Reference:

Xiuli Wu, et al. Design, synthesis and biological evaluation of a series of novel pyrrolo[2,3-d]pyrimidin/pyrazolo[3,4-d]pyrimidin-4-amine derivatives as FGFRs-dominant multi-target receptor tyrosine kinase inhibitors for the treatment of gastric cancer. Bioorg Chem. 2022 Oct;127:105965. doi: 10.1016/j.bioorg.2022.105965. 


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