Capecitabine

Catalog No.S1156 Batch:S115606

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)

Clear solution

5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O

25.0mg/ml

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, 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 (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, 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.

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
Dosages
≤1.5 mM/kg/day
Administration
Administered via p.o.

References

Customer Product Validation

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

: Data independently produced by , , Dr. Helen Sadik of Johns Hopkins University

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

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

Selleck's Capecitabine has been cited by 26 publications

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
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
Establishment and Characterization of NCC-PMP1-C1: A Novel Patient-Derived Cell Line of Metastatic Pseudomyxoma Peritonei [ J Pers Med, 2022, 12(2)258]	PubMed: 35207746
Establishment and characterization of NCC-UPS4-C1: a novel cell line of undifferentiated pleomorphic sarcoma from a patient with Li-Fraumeni syndrome [ Hum Cell, 2022, 10.1007/s13577-022-00671-y]	PubMed: 35118583
Multifocal Organoid Capturing of Colon Cancer Reveals Pervasive Intratumoral Heterogenous Drug Responses [ Adv Sci (Weinh), 2021, e2103360]	PubMed: 34918496
Establishment and characterization of novel patient-derived cell lines from giant cell tumor of bone [ Hum Cell, 2021, 10.1007/s13577-021-00579-z]	PubMed: 34304386
Establishment and characterization of the NCC-GCTB4-C1 cell line: a novel patient-derived cell line from giant cell tumor of bone [ Hum Cell, 2021, 10.1007/s13577-021-00639-4]	PubMed: 34731453
Establishment and characterization of NCC-MFS4-C1: a novel patient-derived cell line of myxofibrosarcoma [ Hum Cell, 2021, 34(6):1911-1918]	PubMed: 34383271
Comprehensive live-cell imaging analysis of cryptotanshinone and synergistic drug-screening effects in various human and canine cancer cell lines [ PLoS One, 2021, 16(2):e0236074]	PubMed: 33544704
Hydrogel-based colorectal cancer organoid co-culture models [ Acta Biomater, 2020, S1742-7061(20)30751-0]	PubMed: 33388439

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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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