Capecitabine 154361-50-9

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Molecular Weight:

359.35 Capecitabine is a tumor-selective fluoropyrimidine carbamate which achieves higher intratumoral 5-FU level with lower toxicity than 5-FU.

Biological Activity

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.


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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