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Capecitabine

CAS No. : 154361-50-9

MCE 国际站：Capecitabine

产品活性：Capecitabine 是一种可用于口服的前体，可由胸苷磷酸化酶催化转变为其活性代谢物 Fluorouracil (FU)。

研究领域：Cell Cycle/DNA Damage  |  Apoptosis

作用靶点：DNA/RNA Synthesis  |  Nucleoside Antimetabolite/Analog  |  Apoptosis

In Vitro: Capecitabine is an anti-cancer chemotherapy drug. It is classified as an antimetabolite. Capecitabine is converted into 5′-deoxy-5-fluorocytidine (5′DFCR), 5′-deoxy-5-fluorouridine (5′DFUR) and 5-FU by carboxylesterases (CES1 and 2), cytidine deaminase (CDD), and thymidine phosphorylase (TP), in both liver and tumour. Capecitabine induces a significant cytotoxic effect in vitro only at high concentrations. Mean IC₅₀ values vary from 860 μM in COLO205 cells to 6000 μM in HCT8 cells.

In Vivo: A pharmacokinetic/pharmacodynamic study is carried out in mice bearing HCT 116 xenografts receiving 0.52 and 2.1 mmol/kg/d of Capecitabine by oral gavage. Capecitabine administered at 0.52 mmol/kg/day induces partial control of HCT 116 xenografts tumour growth: growth rate =7.5±0.5 on day 21. Capecitabine 2.1 mmol/kg/day achieves complete control of tumor growth during the treatment period: growth rate =1±0.2 on day 21.

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