Capecitabine

Catalog No.S1156 Batch:S115606

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Technical Data

Formula

C15H22FN3O6
Molecular Weight 359.35 CAS No. 154361-50-9
Solubility (25°C)* In vitro DMSO 72 mg/mL (200.36 mM)
Ethanol 72 mg/mL (200.36 mM)
Water 18 mg/mL (50.09 mM)
In vivo (Add solvents to the product individually and in order)
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O

Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.

 25.000mg/ml (69.57mM) Taking the 1 mL working solution as an example, add 50 μL of 500 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
* <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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description Capecitabine is a tumor-selective fluoropyrimidine carbamate, which achieves higher intratumoral 5-FU level with lower toxicity than 5-FU. Capecitabine treatment of HCT-15 cells causes condensation of DNA and induces apoptosis.
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, this compound 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.
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. This compound 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.
Features A tumor-selective fluoropyrimidine carbamate.

Protocol (from 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 to this compound, 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

  • Dosages

    ≤1.5 mM/kg/day

  • Administration

    Administered via p.o.

References

  • https://pubmed.ncbi.nlm.nih.gov/12481413/
  • https://pubmed.ncbi.nlm.nih.gov/9605432/
  • https://pubmed.ncbi.nlm.nih.gov/14676129/

Customer Product Validation

<p>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).</p>

, , Cancer Res, 2017, 77(24):7120-7130

<p>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.</p><div><div> </div></div><p> </p>

, , Dr. Helen Sadik of Johns Hopkins University

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.

Data from [ , , Carcinogenesis, 2018, 39(1):72-83 ]

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.

Data from [ , , Mol Carcinog, 2018, 57(10):1383-1395 ]

Selleck's Capecitabine Has Been Cited by 33 Publications

Fisetin and/or capecitabine causes changes in apoptosis pathways in capecitabine-resistant colorectal cancer cell lines [ Naunyn-Schmiedebergs Archives of Pharmacology, May 15, 2024, 7913-7926] PubMed: 30279143
Anti-cancer drug sensitivity testing and preclinical evaluation of the anti-cancer potential of WEE1 inhibitor in triple-negative breast cancer patient-derived organoids and xenograft models [ Breast Cancer Research, June 23, 2025, 113] PubMed: 40551232
A potential novel therapy for FGFR1-amplified pancreatic cancer with bone metastasis, screened by next-generation sequencing and a patient-derived xenograft model [ Oncology Letters, December 28, 2018, 2303-2307]
[18F]fluorothymidine PET Informs the Synergistic Efficacy of Capecitabine and Trifluridine/Tipiracil in Colon Cancer [ Cancer Research, December 15, 2017, 7120-7130]
Individualized drug screening based on next generation sequencing and patient derived xenograft model for pancreatic cancer with bone metastasis [ Molecular Medicine Reports, August 10, 2017, 4784-4790] PubMed: 28849200
A pancreatic cancer organoid biobank links multi-omics signatures to therapeutic response and clinical evaluation of statin combination therapy [ Cell Stem Cell, 2025, S1934-5909(25)00265-6] PubMed: 40812300
Zinc finger protein 831 promotes apoptosis and enhances chemosensitivity in breast cancer by acting as a novel transcriptional repressor targeting the STAT3/Bcl2 signaling pathway [ Genes Dis, 2024, 11(1):430-448] PubMed: 37588209
Patient-derived rhabdomyosarcoma cells recapitulate the genetic and transcriptomic landscapes of primary tumors [ iScience, 2024, 27(10):110862] PubMed: 39319271
Fisetin and/or capecitabine causes changes in apoptosis pathways in capecitabine-resistant colorectal cancer cell lines [ Naunyn Schmiedebergs Arch Pharmacol, 2024, 397(10):7913-7926] PubMed: 38748229
Fisetin and/or capecitabine causes changes in apoptosis pathways in capecitabine-resistant colorectal cancer cell lines [ Naunyn Schmiedebergs Arch Pharmacol, 2024, 10.1007/s00210-024-03145-0] PubMed: 38748229

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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