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
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Cited by 5 Publications

6 Customer Reviews

  • Growth curve of human colon cancer xenografts in nude mice treated with orally administered vehicle or capecitabine at 360 mg/kg (n = 10–12 per cell line).

    Cancer Res, 2017, 77(24):7120-7130. Capecitabine purchased from Selleck.

    A452 induces apoptosis and DNA damage of CRC cells. (A) HCT116 and (B) HT29 cells were cultured with 0.1% DMSO (control) or A452 (0.5, 1, 2 uM), SAHA (5 uM), cisplatin (10 uM), irinotecan (5 uM), or capecitabine (10 uM) at the indicated concentrations for 24 h. The Western blot analysis shows PARP degradation, proapoptotic and antiapoptotic markers. α-Tubulin is shown as a loading control.

    Carcinogenesis, 2018, 39(1):72-83. Capecitabine purchased from Selleck.

  • A, HCT116 and (B) HT29 cells were treated with 0.1% DMSO (control), A452 (2 µM), SAHA (5 µM), cisplatin (10 µM), irinotecan (5 µM), or capecitabine (10 µM) alone or in combination with these compounds at the indicated concentrations for 24 h. The total protein was analyzed by western blotting with α‐tubulin as a loading control.

    Mol Carcinog, 2018, 57(10):1383-1395. Capecitabine purchased from Selleck.

    Live Dead Assay fluorescent microscopic images of C6 colon cancer cells exposed to (A) free drug Cap for 24 h, (B) PLGA Cap NPs for 24 h, (C) free drug Cap for 150 h, and (D) PLGA Cap NPs for 150 h.

    J Drug Deliv Sci Tec, 2018, doi:10.1016/j.jddst.2018.05.025. Capecitabine purchased from Selleck.

  • (A) Antitumor-growth ability of AZD6244. (B) The single AZD6244 exhibited better efficacy than Capecitabine, while the combination of both shown a significant synergistic effect.

    Mol Med Rep, 2017, 16(4):4784-4790. Capecitabine purchased from Selleck.

    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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Biological Activity

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 NEnLbXNEgXSxdH;4bYPDqGG|c3H5 Mn:2N{Bl[Xm| NYni[IFKS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hWkuRcEK3JINmdGy|IHHmeIVzKDNiZHH5d{BjgSCPVGSgZZN{[XluIFnDOVA:PC5|MzFOwG0> MXmyNFM2PjZ3NR?=

... 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
in solvent
Synonyms RO 09-1978

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03818685 Not yet recruiting Breast Cancer|Triple Negative Breast Neoplasms Centre Leon Berard April 1 2019 Phase 2
NCT03818685 Not yet recruiting Breast Cancer|Triple Negative Breast Neoplasms Centre Leon Berard April 1 2019 Phase 2
NCT03869892 Not yet recruiting Metastatic Colorectal Cancer Institut de Recherches Internationales Servier|ADIR a Servier Group company|Servier March 20 2019 Phase 3
NCT03813784 Not yet recruiting Gastric Cancer|GastroEsophageal Cancer Jiangsu HengRui Medicine Co. Ltd. March 2019 Phase 3
NCT03770689 Not yet recruiting Locally Advanced Rectal Cancer EMD Serono Research & Development Institute Inc.|Merck KGaA Darmstadt Germany|EMD Serono March 4 2019 Phase 1|Phase 2
NCT03873532 Not yet recruiting Biliary Tract Cancer Hutchison Medipharma Limited March 2019 Phase 2|Phase 3

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID