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

Capecitabine 

Cat. No.: HY-B0016 Purity: 99.97%
Handling Instructions

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

For research use only. We do not sell to patients.

Capecitabine Chemical Structure

Capecitabine Chemical Structure

CAS No. : 154361-50-9

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Based on 2 publication(s) in Google Scholar

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Description

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

IC50 & Target

DNA/RNA Synthesis[1]

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].

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].

Clinical Trial
Molecular Weight

359.35

Formula

C₁₅H₂₂FN₃O₆

CAS No.

154361-50-9

SMILES

C[[email protected]@H]1[[email protected]]([[email protected]]([[email protected]](N2C(N=C(C(F)=C2)NC(OCCCCC)=O)=O)O1)O)O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (278.28 mM; Need ultrasonic)

H2O : ≥ 33.33 mg/mL (92.75 mM)

*"≥" means soluble, but saturation unknown.

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
10 mM 0.2783 mL 1.3914 mL 2.7828 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

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

    Solubility: ≥ 10 mg/mL (27.83 mM); Clear solution

  • 2.

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

    Solubility: ≥ 10 mg/mL (27.83 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 10 mg/mL (27.83 mM); Clear solution

*All of the co-solvents are provided by MCE.
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

Purity: 99.97%

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Keywords:

CapecitabineDNA/RNA SynthesisApoptosisNucleoside Antimetabolite/AnalogInhibitorinhibitorinhibit

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Product name:
Capecitabine
Cat. No.:
HY-B0016
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