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抑制劑描述：

產(chǎn)品名稱(chēng)：Capecitabine

產(chǎn)品別名：卡培他濱

英文別名：Capecitabine

靶點(diǎn)：Thymidine phosphorylase

CAS：154361-50-9

純度：>98%

外觀：白色至類(lèi)白色結(jié)晶性粉末

保存方法：store at -20℃ for one year（Powder）； in DMSO or others solvent store at 2-4℃ for two weeks, at -20℃ for six months.

描述：

Prodrug of 5-Fluorouracil (5-FU). Selectively activated in tumor cells by thymidine phosphorylase; inhibits DNA synthesis upon conversion to 5-FU. Orally available.

溶解性：Ethanol ：35.9 mg/mL (100 mM)
DMSO ：35.9 mg/mL (100 mM)

體外研究：

Both LS174T WT and LS174T-c2 cells show significantly greater sensitivity to Capecitabine when cultivated in the same plates as HepG2 hepatoma with IC50 values of 890 and 630 μM in LS174T WT alone and cultivated with HepG2, respectively. In addition, for the LS174T-C2 subline, the IC50 falls from 330 ± 4 down to 89 ± 6 μm when cultivated in the same plates as hepatoma cells. Furthermore, Capecitabine induces apoptosis in a Fas-dependent manner, and shows a 7-fold higher cytotoxicity and markedly stronger apoptotic potential in thymidine phosphorylase (TP)-transfected LS174T-c2 cells.

體內(nèi)研究：In the human cancer xenograft models studied, Capecitabine is more effective in a wider dose range and has a broader spectrum of antitumor activity than 5-FU, UFT or its intermediate metabolite 5'-DFUR, which can be correlated with tumor dThdPase levels. Capecitabine inhibits tumor growth and metastatic recurrence after resection of human hepatocellular carcinoma (HCC) in highly metastatic nude mice model which is attributed to the high expression of platelet-derived endothelial cell growth factor in tumors.

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