2. Cell Cycle/DNA Damage Apoptosis
  3. DNA/RNA Synthesis Nucleoside Antimetabolite/Analog Apoptosis
  4. Capecitabine

Capecitabine is an oral proagent that is converted to its active metabolite, 5-FU, by thymidine phosphorylase.

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CAS No. : 154361-50-9

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Based on 29 publication(s) in Google Scholar

Other Forms of Capecitabine:

Capecitabine Related Antibodies

Top Publications Citing Use of Products

29 Publications Citing Use of MCE Capecitabine

In Vivo Efficacy Study
Histological Imaging/Staining
IHC
WB
Cell Proliferation/Viability Assay

    Capecitabine purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2025 Jan 31:e2408845.  [Abstract]

    Dose-response curves of HCT116 to Capecitabine (0-100 μM; 24 h).

    Capecitabine purchased from MedChemExpress. Usage Cited in: J Clin Invest. 2024 Mar 7;134(10):e172716.  [Abstract]

    The given cell lines were treated with 250 nM osimertinib (Osim), 1.25 μM Etoposide (VP-16), 125 nM Doxorubicin (DXR), 5 nM Paclitaxel, 10 μM Cisplatin, 25 μM Carboplatin, 25 nM Gemcitabine, 20 nM 5-Fluorouracil (5-FU), 25 μM Cyclophosphamide, 25 μM Capecitabine, or 10 nM Vincristine alone or in combination for 3 days. Cell numbers were then measured using the SRB assay.

    Capecitabine purchased from MedChemExpress. Usage Cited in: J Adv Res. 2021 Jun 12:36:265-276.

    Ginsenoside Compound K (GCK) and Capecitabine (359 mg/kg; i.g.; 5 days/week for 3 weeks and stop for 1 week) inhibited the growth of xenograft tumors.

    Capecitabine purchased from MedChemExpress. Usage Cited in: J Adv Res. 2021 Jun 12:36:265-276.

    H&E staining to detect tumor necrosis in mice models treated with Ginsenoside Compound K (GCK) and Capecitabine (359 mg/kg; i.g.; 5 days/week for 3 weeks and stop for 1 week) .

    Capecitabine purchased from MedChemExpress. Usage Cited in: J Adv Res. 2021 Jun 12:36:265-276.

    IHC detected the expression of Ki-67 in tumor tissue of mice models treated with Ginsenoside Compound K (GCK) and Capecitabine (359 mg/kg; i.g.; 5 days/week for 3 weeks and stop for 1 week) .

    Capecitabine purchased from MedChemExpress. Usage Cited in: J Adv Res. 2021 Jun 12:36:265-276.

    Ginsenoside Compound K (GCK) and Capecitabine (359 mg/kg; i.g.; 5 days/week for 3 weeks and stop for 1 week) decreased the protein expressions of N-cadherin, ZEB1, MMP-9, MMP-2 and Vimentin in vivo.

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    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Capecitabine is an oral proagent that is converted to its active metabolite, 5-FU, by thymidine phosphorylase.

    IC50 & Target

    DNA/RNA Synthesis[1]
    Cellular Effect
    Cell Line Type Value Description References
    HCT-116 IC50
    34.2 μM
    Compound: Cape
    Antiproliferative activity against human HCT-116 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
    Antiproliferative activity against human HCT-116 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
    		[PMID: 35300092]
    HeLa IC50
    0.05 mg/mL
    Compound: 4a, Capecitabine
    Cytotoxicity against human HeLa cells after 3 days MTT assay
    Cytotoxicity against human HeLa cells after 3 days MTT assay
    		[PMID: 22796042]
    KG-1 IC50
    8.9 μM
    Compound: Cape
    Antiproliferative activity against human KG-1 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
    Antiproliferative activity against human KG-1 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
    		[PMID: 35300092]
    MCF7 IC50
    0.71 mg/mL
    Compound: 4a, Capecitabine
    Cytotoxicity against human MCF7 cells after 3 days MTT assay
    Cytotoxicity against human MCF7 cells after 3 days MTT assay
    		[PMID: 22796042]
    NCI-H69 IC50
    0.3 mg/mL
    Compound: 4a, Capecitabine
    Cytotoxicity against human NCI-H69 cells after 3 days MTT assay
    Cytotoxicity against human NCI-H69 cells after 3 days MTT assay
    		[PMID: 22796042]
    In Vitro

    Capecitabine is an anti-cancer chemotherapy drug. It is classified as an antimetabolite. Capecitabine is converted into 5′-deoxy-5-fluorocytidine (5′DFCR), 5′-deoxy-5-fluorouridine (5′DFUR) and 5-FU by carboxylesterases (CES1 and 2), cytidine deaminase (CDD), and thymidine phosphorylase (TP), in both liver and tumour. Capecitabine induces a significant cytotoxic effect in vitro only at high concentrations. Mean IC50 values vary from 860 μM in COLO205 cells to 6000 μM in HCT8 cells[2].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    Capecitabine Related Antibodies
    In Vivo

    A pharmacokinetic/pharmacodynamic study is carried out in mice bearing HCT 116 xenografts receiving 0.52 and 2.1 mmol/kg/d of Capecitabine by oral gavage. Capecitabine administered at 0.52 mmol/kg/day induces partial control of HCT 116 xenografts tumour growth: growth rate =7.5±0.5 on day 21. Capecitabine 2.1 mmol/kg/day achieves complete control of tumor growth during the treatment period: growth rate =1±0.2 on day 21[2].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
    Clinical Trial
    Molecular Weight

    359.35

    Formula

    C15H22FN3O6
    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    O[C@H]1[C@@H](O)[C@H](N2C=C(C(NC(OCCCCC)=O)=NC2=O)F)O[C@@H]1C
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 1 year
    -20°C 6 months
    Solvent & Solubility
    In Vitro: 

    DMSO : 250 mg/mL (695.70 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    H2O : 12.5 mg/mL (34.79 mM; ultrasonic and warming and heat to 60°C)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.7828 mL 13.9140 mL 27.8280 mL
    5 mM 0.5566 mL 2.7828 mL 5.5656 mL
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

    * Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

    • Molarity Calculator

    • Dilution Calculator

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    Mass
    =
    Concentration
    ×
    Volume
    ×
    Molecular Weight *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

    ×
    Volume (final)

    V2

    In Vivo:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.08 mg/mL (5.79 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • Protocol 2

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.08 mg/mL (5.79 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

      Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.

    For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  50% PEG300    50% Saline

      Solubility: 20 mg/mL (55.66 mM); Clear solution; Need ultrasonic

    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    Purity & Documentation

    Purity: 99.99%

    SDS (419 KB)

    COA (246 KB) LCMS (93 KB)

    Handling Instructions (2659 KB)
    References
    Cell Assay
    [2]

    HCT 116, HCT8, HCT15, HT29, SW620 and COLO205 human colon cancer cells are used. Cells are plated on day 1 in 96-well plates at a density of 2500 cells/well for HCT 116, 3500 cells/well for HCT8 and HT29, 5000 cells/well for HCT15, 6000 cells/well for SW620 and 7000 cells/wells for COLO205 in a volume of 150 μL/well. All cell lines are treated on day 2 with increasing concentrations of Capecitabine (0.1-10 mM), 5′DFCR (10 nM-100 μM), 5′DFUR (2.5-500 μM) or 5-FU (0.5-250 μM) for 24 h. After drug exposure, cells are washed once with cold PBS and placed in 200 μL of drug-free medium for 72 h after the end of drug exposure. The cells are then fixed with trichloroacetic acid and stained with sulforhodamine B. Optical densities are measured at 540 nm with a Biohit BP-800. The results are based on three independent experiments performed in triplicate[2].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Animal Administration
    [2]

    Mice[2]
    Six-week-old C57/Bl6 Nu/Nu mice are used. Bilateral HCT 116 xenografts are obtained by subcutaneous injection of 107 cells/flank. Animals bearing HCT 116 xenografts are treated with vehicle or Capecitabine 0.52 or 2.1 mmol/kg (563 and 2250 mg/m2, respectively) given once daily for 5 consecutive days/week by oral gavage for 3 weeks (days 0-4, 7-11, 14-18). Animals are culled on day 0 at 15, 30 min, 1, 2, 4, 8 and 24 h, and prior to planned treatment on days 7 and 14 after the start of treatment. Three animals per time-point are analysed. At the time of collection, blood is collected in heparin, and plasma isolated and stored at −80°C. The liver is removed immediately and stored in RNAlater solution. Tumours are macro-dissected to remove fibrotic tissue and blood vessels and snap-frozen in liquid nitrogen.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    References

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    H2O / DMSO 1 mM 2.7828 mL 13.9140 mL 27.8280 mL 69.5701 mL
    5 mM 0.5566 mL 2.7828 mL 5.5656 mL 13.9140 mL
    10 mM 0.2783 mL 1.3914 mL 2.7828 mL 6.9570 mL
    15 mM 0.1855 mL 0.9276 mL 1.8552 mL 4.6380 mL
    20 mM 0.1391 mL 0.6957 mL 1.3914 mL 3.4785 mL
    25 mM 0.1113 mL 0.5566 mL 1.1131 mL 2.7828 mL
    30 mM 0.0928 mL 0.4638 mL 0.9276 mL 2.3190 mL
    DMSO 40 mM 0.0696 mL 0.3479 mL 0.6957 mL 1.7393 mL
    50 mM 0.0557 mL 0.2783 mL 0.5566 mL 1.3914 mL
    60 mM 0.0464 mL 0.2319 mL 0.4638 mL 1.1595 mL
    80 mM 0.0348 mL 0.1739 mL 0.3479 mL 0.8696 mL
    100 mM 0.0278 mL 0.1391 mL 0.2783 mL 0.6957 mL

    * Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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    Capecitabine Related Classifications

    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    Capecitabine154361-50-9DNA/RNA SynthesisNucleoside Antimetabolite/AnalogApoptosisInhibitorinhibitorinhibit

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