Home DNA Damage/DNA Repair DNA/RNA Synthesis inhibitor - Apoptosis related activator Capecitabine For research use only.

Capecitabine

Synonyms: RO 09-1978

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.

Capecitabine Chemical Structure

Capecitabine Chemical Structure

CAS No. 154361-50-9

Purity & Quality Control

Capecitabine Related Products

Signaling Pathway

DNA/RNA Synthesis Signaling Pathways

DNA/RNA Synthesis Signaling Pathway

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human RKOp27 cells Cytotoxic assay 3 days Cytotoxicity against human RKOp27 cells after 3 days by MTT assay, IC50=4.33 μM 20356655
RKOp27 Cytotoxicity assay Cytotoxicity against human RKOp27 cells by MTT assay, IC50 = 0.00433 μM. 19345581
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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.
Features A tumor-selective fluoropyrimidine carbamate.
Targets
Thymidine phosphorylase [1]
In vitro
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]
Cell Research 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.
In Vivo
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]
Animal Research 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.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT06247995 Not yet recruiting
Breast Cancer
Novartis Pharmaceuticals|Novartis
 May 16 2024 Phase 1|Phase 2
NCT06085742 Recruiting
Breast Cancer
University of Illinois at Chicago
 November 22 2023 Phase 2
NCT05929885 Recruiting
Metastatic Pancreatic Cancer
National Cancer Centre Singapore|National Medical Research Council (NMRC) Singapore
 August 30 2023 Phase 2

Chemical Information & Solubility

Molecular Weight 359.35 Formula

C15H22FN3O6
CAS No. 154361-50-9 SDF Download Capecitabine SDF
Smiles CCCCCOC(=O)NC1=NC(=O)N(C=C1F)C2C(C(C(O2)C)O)O
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 72 mg/mL ( (200.36 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 72 mg/mL

Water : 6 mg/mL


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