Capecitabine

Description

Description

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

In vitro

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. ^[1]

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. ^[2] 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. ^[3]

A tumor-selective fluoropyrimidine carbamate.

Capecitabine

Catalog No.S1156

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

Size

Price

Stock

Quantity

10mM/1mLIn DMSO	USD 604	In stock	0 1 2 3 4 5 6 7 8 9 10
50mg	USD 122	In stock	0 1 2 3 4 5 6 7 8 9 10

Distributor Tel: +886-2-2827-1197jimmy@new.abscience.com.tw

Cell lines	HepG2, LS174T WT and LS174T-c2 cells
Concentrations	~1 mM
Incubation Time	72 hours
Method	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.

Animal Models	BALB/c nu/nu mice are inoculated s.c. with small pieces of CXF280 xenograft tissues
Dosages	≤1.5 mM/kg/day
Administration	Administered via p.o.
Solubility	30% propylene glycol, 5% Tween 80, 65% D5W, 30 mg/mL

Solubility (25°C) *	In vitro	DMSO	72 mg/mL (200 mM)
		Water	6 mg/mL (16 mM)
		Ethanol	72 mg/mL (200 mM)
	In vivo	30% propylene glycol, 5% Tween 80, 65% D5W,	30 mg/mL
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Name	pentyl 1-((2R,3R,4S,5R)-3,4-dihydroxy-5-methyl-tetrahydrofuran-2-yl)-5-fluoro-2-oxo-1,2-dihydropyrimidin-4-ylcarbamate

Stock Solution (1ml DMSO)	1mM	10mM	20mM	30mM
Mass(mg)	0.35935	3.5935	7.187	10.7805

Click to enlarge	Rating
	Source	Dr. Helen Sadik of Johns Hopkins University. Capecitabine purchased from Selleck
	Method	MTT assay
	Cell Lines	MCF7 cells, MCF10A cells
	Concentrations	0.001-100 μM
	Incubation Time	48 h
	Results	Capecitabine potently inhibited the survival of MCF10A cells and MCF7 cells in a dose-dependent manner.