Capecitabine

Catalog No.S1156
4 5

Capecitabine is a tumor-selective fluoropyrimidine carbamate which achieves higher intratumoral 5-FU level with lower toxicity than 5-FU.

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In DMSO USD 480 In stock
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Capecitabine  Chemical Structure

Capecitabine Chemical Structure
Molecular Weight: 359.35

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Quality Control & MSDS

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Product Information

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Product Description

Biological Activity

Description Capecitabine is a tumor-selective fluoropyrimidine carbamate which achieves higher intratumoral 5-FU level with lower toxicity than 5-FU.
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(Only for 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
Formulation Capecitabine is dissolved in water.
Dosages ≤1.5 mM/kg/day
Administration Administered via p.o.
Solubility 30% propylene glycol, 5% Tween 80, 65% D5W, 30 mg/mL
* 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.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesBaboonDogMonkeyRabbitGuinea pigRatHamsterMouse
Weight (kg)121031.80.40.150.080.02
Body Surface Area (m2)0.60.50.240.150.050.0250.020.007
Km factor202012128653
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

References

[1] Ciccolini J, et al. Mol Cancer Ther. 2002, 1(11), 923-927.

[2] Ishikawa T, et al. Biochem Pharmacol. 1998, 55(7), 1091-1097.

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Clinical Trial Information( data from http://clinicaltrials.gov, updated on 2014-10-24)

NCT Number Recruitment Conditions Sponsor
/Collaborators
Start Date Phases
NCT02121405 Not yet recruiting Colorectal Neoplasm|Effects of Radiation Therapy|Effects of Chemotherapy|Surgery Zhejiang University December 2014 Phase 3
NCT01972919 Not yet recruiting Unresectable Pancreatic Cancer Medical College of Wisconsin December 2014 Phase 1|Phase 2
NCT02205047 Not yet recruiting Malignant Neoplasm of Stomach|Malignant Neoplasm of Cardio-esophageal Junction of Stomach|Epidermal Growth Factor Receptor (EGFR) Protein Overexpre  ...more Malignant Neoplasm of Stomach|Malignant Neoplasm of Cardio-esophageal Junction of Stomach|Epidermal Growth Factor Receptor (EGFR) Protein Overexpression European Organisation for Research and Treatment of Cance  ...more European Organisation for Research and Treatment of Cancer - EORTC December 2014 Phase 2
NCT02025036 Not yet recruiting Stage III Esophageal Squamous Cell Carcinoma|Stage II Esophageal Squamous Cell Carcinoma The First Affiliated Hospital of Henan University of Scie  ...more The First Affiliated Hospital of Henan University of Science and Technology October 2014 Phase 3
NCT00960544 Not yet recruiting Breast Cancer M.D. Anderson Cancer Center|Myriad Genetic Laboratories,  ...more M.D. Anderson Cancer Center|Myriad Genetic Laboratories, Inc. October 2014 Phase 2

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Chemical Information

Download Capecitabine SDF
Molecular Weight (MW) 359.35
Formula

C15H22FN3O6

CAS No. 154361-50-9
Storage 3 years -20℃Powder
6 months-80℃in DMSO
Synonyms
Solubility (25°C) * In vitro DMSO 72 mg/mL (200 mM)
Water 6 mg/mL (16 mM)
Ethanol 72 mg/mL (200 mM)
In vivo 30% propylene glycol, 5% Tween 80, 65% D5W 30 mg/mL
* <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.
Chemical Name pentyl 1-((2R,3R,4S,5R)-3,4-dihydroxy-5-methyl-tetrahydrofuran-2-yl)-5-fluoro-2-oxo-1,2-dihydropyrimidin-4-ylcarbamate

Research Area

Customer Reviews (1)


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Rating
Source Dr. Helen Sadik of Johns Hopkins University. Capecitabine purchased from Selleck
Method MTT assay
Cell Lines MCF7 cells, MCF10A cells
Concentrations 0.001-100 μM
Incubation Time 48 h
Results Capecitabine potently inhibited the survival of MCF10A cells and MCF7 cells in a dose-dependent manner.

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