product name Capecitabine
Description: Capecitabine (also known as RO 09-1978) is an anti-cancer chemotherapy drug of the fluoropyrimidine carbamate class, it has higher intratumoral 5-FU level with lower toxicity than 5-FU. In antiproliferative assays, both LS174T WT and LS174T-c2 cells were more sensitive to capecitabine when cultivated in the same plates as HepG2 hepatoma. In LS174T WT alone and cultivated with HepG2, IC50 values of capecitabine were 890 ± 48 and 630 ± 14 μm respectively.
References: Mol Cancer Ther. 2002 Sep;1(11):923-7; Biochem Pharmacol. 1998 Apr 1;55(7):1091-7.
359.35
Formula
C15H22FN3O6
CAS No.
154361-50-9
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 72 mg/mL (200.4 mM)
Water: 6 mg/mL (16.7 mM)
Ethanol: 72 mg/mL (200.4 mM)
Solubility (In vivo)
Synonyms
RO 09-1978
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19412756
| In Vitro |
In vitro 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. Kinase Assay: Cell Assay: HepG2 and either LS174T WT or LS174T-c2 cells are seeded, respectively, in the top and bottom chambers of 8-well strip membranes in 96-well plates. The exponentially growing cells are exposed to increasing concentrations of capecitabine. The medium is supplemented with 750 ng/mL ZB4 MoAB or 100 ng/mL BR17 MoAB when the latter are used in the experiments. After 72 hours of continuous exposure, LS174T viability is assessed using the classic colorimetric MTT test. |
|---|---|
| In Vivo | 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. |
| Animal model | BALB/c nu/nu mice are inoculated s.c. with small pieces of CXF280 xenograft tissues |
| Formulation & Dosage | Dissolved in water; ≤1.5 mM/kg/day; p.o. |
| References | Mol Cancer Ther. 2002 Sep;1(11):923-7; Biochem Pharmacol. 1998 Apr 1;55(7):1091-7. |
