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設(shè)計(jì)合成一系列用于治療胃癌的多靶點(diǎn)受體酪氨酸激酶抑制劑,并進(jìn)行生物學(xué)評價(jià)。其中藥代動力學(xué)分析通過美迪西進(jìn)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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