Capecitabine

Catalog No.S1156
1 Reviews

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

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In DMSO USD 480 In stock
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Capecitabine  Chemical Structure

Capecitabine Chemical Structure
Molecular Weight: 359.35

Validation & Quality Control

Customer Reviews(1)

Quality Control & MSDS

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Product Information

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Product Description

Biological Activity

Description Capecitabine is a tumor-selective fluoropyrimidine carbamate which achieves higher intratumoral 5-FU level with lower toxicity than 5-FU.
Targets Thymidine phosphorylase
IC50 [1]()
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 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. [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]
Features A tumor-selective fluoropyrimidine carbamate.

Protocol(Only for Reference)

Cell Assay: [1]

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 Study: [2]

Animal Models BALB/c nu/nu mice are inoculated s.c. with small pieces of CXF280 xenograft tissues
Formulation Capecitabine is dissolved in water.
Dosages ≤1.5 mM/kg/day
Administration Administered via p.o.
Solubility 30% propylene glycol, 5% Tween 80, 65% D5W, , 30 mg/mL
* 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.
1

References

[1] Ciccolini J, et al. Mol Cancer Ther. 2002, 1(11), 923-927.

[2] Ishikawa T, et al. Biochem Pharmacol. 1998, 55(7), 1091-1097.

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Clinical Trial Information( data from http://clinicaltrials.gov)

NCT Number Recruitment Conditions Sponsor
/Collaborators
Start Date Phases
NCT00960544 Not yet recruiting Breast Cancer M.D. Anderson Cancer Center|Myriad Genetic Laboratories, Inc. 2014-03 Phase 2
NCT02028507 Recruiting Metastatic Breast Cancer Spanish Breast Cancer Research Group|Pfizer 2014-03 Phase 3
NCT02000882 Not yet recruiting Triple Negative Breast Cancer|Brain Metastases|Breast Cancer US Oncology Research|Novartis Pharmaceuticals 2014-04 Phase 2
NCT02089633 Recruiting Hepatocellular Carcinoma Bio-Cancer Treatment International Limited|The University of Hong Kong 2014-04 Phase 2
NCT02024009 Not yet recruiting Locally Advanced Non-metastatic Pancreatic Cancer Cardiff University|Lisette Nixon|Celgene Corporation|Cancer Research UK 2014-06 Phase 2|Phase 3

Chemical Information

Download Capecitabine SDF
Molecular Weight (MW) 359.35
Formula

C15H22FN3O6

CAS No. 154361-50-9
Storage 3 years -20℃Powder
6 months-80℃in DMSO
Synonyms
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

Research Area

Customer Reviews (1)


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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.

Tech Support & FAQs

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