Capecitabine (RO 09-1978)

Catalog No.S1156

For research use only.

Capecitabine (RO 09-1978) 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 (RO 09-1978) Chemical Structure

CAS No. 154361-50-9

Selleck's Capecitabine (RO 09-1978) has been cited by 21 publications

Purity & Quality Control

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Biological Activity

Description Capecitabine (RO 09-1978) 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

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 Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human RKOp27 cells NF61WHhEgXSxdH;4bYPDqGG|c3H5 MlXKN{Bl[Xm| MlvRR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gVmtQeDJ5IHPlcIx{KGGodHXyJFMh\GG7czDifUBOXFRiYYPzZZktKEmFNUC9OE4{OyEQvF2= MV:8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zODN3Nk[1OUc,OjB|NU[2OVU9N2F-
RKOp27 NWHpZnU2S3m2b4TvfIlkcXS7IHHzd4F6 M3jpfWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJHJMV3B{NzDj[YxteyCkeTDNWHQh[XO|YYmsJGlEPTBiPTCwMlAxPDN|IN88UU4> MnTpQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTl|NEW1PFEoRjF7M{S1OVgyRC:jPh?=
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]

Protocol (from reference)

Cell Research:[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 Research:[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.

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 359.35
Formula

C15H22FN3O6

CAS No. 154361-50-9
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CCCCCOC(=O)NC1=NC(=O)N(C=C1F)C2C(C(C(O2)C)O)O

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Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT05348278 Recruiting Drug: Urea cream Hand-Foot Syndrome Mahidol University|Siriraj Hospital December 20 2021 Phase 2|Phase 3
NCT05093907 Recruiting Drug: BEY1107|Combination Product: Capecitabine Metastatic Colorectal Cancer BeyondBio Inc. August 31 2021 Phase 1|Phase 2
NCT04861987 Recruiting Drug: PCS6422 and capecitabine Advanced Cancer|Refractory Cancer|Tumor Gastric Processa Pharmaceuticals June 18 2021 Phase 1

(data from https://clinicaltrials.gov, updated on 2022-08-01)

Tech Support

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