Capecitabine

Catalog No.S1156 Synonyms: RO 09-1978

Capecitabine  Chemical Structure

Molecular Weight(MW): 359.35

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

Size Price Stock Quantity  
In DMSO USD 137 In stock
USD 97 In stock
USD 297 In stock
USD 670 In stock
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1 Customer Review

  • Cells were seeded in 96 well paltes, and then treated with the indicated concentration of Capecitabine for 48 h. Cell survival was measured by a standarad MTT assay.

     

     

    Dr. Helen Sadik of Johns Hopkins University. Capecitabine purchased from Selleck.

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

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human RKOp27 cells MY\DfZRwfG:6aXRCpIF{e2G7 NWq3dYxqOyCmYYnz NWLNdZNqS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hWkuRcEK3JINmdGy|IHHmeIVzKDNiZHH5d{BjgSCPVGSgZZN{[XluIFnDOVA:PC5|MzFOwG0> MVKyNFM2PjZ3NR?=

... Click to View More Cell Line Experimental Data

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]

Protocol

Cell Research:[1]
+ Expand
  • 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.
    (Only for Reference)
Animal Research:[2]
+ Expand
  • 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.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 72 mg/mL (200.36 mM)
Ethanol 72 mg/mL (200.36 mM)
Water 6 mg/mL (16.69 mM)

* 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 Information

Molecular Weight 359.35
Formula

C15H22FN3O6

CAS No. 154361-50-9
Storage powder
Synonyms RO 09-1978

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02393755 Recruiting Colon Adenocarcinoma|Rectal Adenocarcinoma|Recurrent Colon Carcinoma|Recurrent Rectal Carcinoma|Stage IVA Colon Cancer|Stage IVA Rectal Cancer|Stage IVB Colon Cancer|Stage IVB Rectal Cancer Roswell Park Cancer Institute|National Cancer Institute (NCI)|Boehringer Ingelheim|National Comprehensive Cancer Network May 8, 2015 Phase 1|Phase 2
NCT02352831 Recruiting Pancreatic Cancer|Cancer of Pancreas|Cancer of the Pancreas|Pancreas Cancer Washington University School of Medicine August 31, 2015 Phase 1|Phase 2
NCT03050814 Not yet recruiting Colorectal Cancer National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) February 3, 2017 Phase 2
NCT01497392 Completed Adenocarcinoma of the Pancreas|Stage III Pancreatic Cancer|Stage IV Pancreatic Cancer|Unspecified Adult Solid Tumor, Protocol Specific Roswell Park Cancer Institute|National Cancer Institute (NCI)|Novartis March 29, 2012 Phase 1
NCT01134601 Terminated Non-Metastatic Adenocarcinoma of the Rectum National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) May 24, 2010 Phase 1
NCT02954055 Not yet recruiting Breast Cancer International Breast Cancer Study Group May 2017 Phase 2

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID