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Capecitabine

Capecitabine
Capecitabine (Capecitibine) is a fluoropyrimidine carbamate belonging to the class of antineoplastic agents called antimetabolites. As a prodrug, capecitabine is selectively activated by tumor cells to its cytotoxic moiety, 5-fluorouracil (5-FU); subsequently, 5-FU is metabolized to two active metabolites, 5-fluoro-2-deoxyuridine monophosphate (FdUMP) and 5-fluorouridine triphosphate (FUTP) by both tumor cells and normal cells. FdUMP inhibits DNA synthesis and cell division by reducing normal thymidine production, while FUTP inhibits RNA and protein synthesis by competing with uridine triphosphate for incorporation into the RNA strand.
Catalog No. T1408Cas No. 154361-50-9
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Capecitabine

Catalog No. T1408Cas No. 154361-50-9

Capecitabine (Capecitibine) is a fluoropyrimidine carbamate belonging to the class of antineoplastic agents called antimetabolites. As a prodrug, capecitabine is selectively activated by tumor cells to its cytotoxic moiety, 5-fluorouracil (5-FU); subsequently, 5-FU is metabolized to two active metabolites, 5-fluoro-2-deoxyuridine monophosphate (FdUMP) and 5-fluorouridine triphosphate (FUTP) by both tumor cells and normal cells. FdUMP inhibits DNA synthesis and cell division by reducing normal thymidine production, while FUTP inhibits RNA and protein synthesis by competing with uridine triphosphate for incorporation into the RNA strand.
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Pack SizePriceAvailabilityQuantity
500 mg$46In Stock
1 g$62In Stock
5 g$163In Stock
1 mL x 10 mM (in DMSO)$48In Stock
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Product Introduction

Bioactivity
Description
Capecitabine (Capecitibine) is a fluoropyrimidine carbamate belonging to the class of antineoplastic agents called antimetabolites. As a prodrug, capecitabine is selectively activated by tumor cells to its cytotoxic moiety, 5-fluorouracil (5-FU); subsequently, 5-FU is metabolized to two active metabolites, 5-fluoro-2-deoxyuridine monophosphate (FdUMP) and 5-fluorouridine triphosphate (FUTP) by both tumor cells and normal cells. FdUMP inhibits DNA synthesis and cell division by reducing normal thymidine production, while FUTP inhibits RNA and protein synthesis by competing with uridine triphosphate for incorporation into the RNA strand.
In vitro
When administered to mice with a high propensity for liver metastasis, Capecitabine exhibits inhibitory effects on both the growth and metastatic recurrence of human hepatocellular carcinoma. This phenomenon is attributed to the high expression of platelet-driven endothelial growth factor within the tumors. Compared to 5-FU, UFT, and the intermediate metabolite 5'-DFUR, Capecitabine demonstrates a broader spectrum of anticancer activity against human transplant tumors, which is associated with the tumor levels of dThdPase.
In vivo
Capecitabine induces apoptosis in a Fas-dependent manner and exhibits toxicity sevenfold higher towards LS174T-c2 cells, which are transfected with thymidine phosphorylase, leading to more pronounced apoptosis. When cultured in the same plate as HepG2 cells, both LS174TWT and LS174T-c2 cells show increased sensitivity to Capecitabine, with IC50 values decreasing from 890 μM when LS174TWT cells are cultured alone to 630 μM when co-cultured with HepG2 cells. Additionally, for the LS174T-C2 subtype co-cultured with HepG2 cells, the IC50 significantly drops from 330±4 μM to 89±6 μM.
Cell Research
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.(Only for Reference)
AliasXeloda, Capecitibine, Capiibine, RO 09-1978
Chemical Properties
Molecular Weight359.35
FormulaC15H22FN3O6
Cas No.154361-50-9
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
5% DMSO+95% Saline: 1.8 mg/mL (5 mM), Working solution is recommended to be prepared and used immediately.
Ethanol: 35.9 mg/mL (100 mM)
DMSO: 35.9 mg/mL (100 mM)
Solution Preparation Table
5% DMSO+95% Saline/Ethanol/DMSO
1mg5mg10mg50mg
1 mM2.7828 mL13.9140 mL27.8280 mL139.1401 mL
5 mM0.5566 mL2.7828 mL5.5656 mL27.8280 mL
Ethanol/DMSO
1mg5mg10mg50mg
10 mM0.2783 mL1.3914 mL2.7828 mL13.9140 mL
20 mM0.1391 mL0.6957 mL1.3914 mL6.9570 mL
50 mM0.0557 mL0.2783 mL0.5566 mL2.7828 mL
100 mM0.0278 mL0.1391 mL0.2783 mL1.3914 mL

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