Catalog No.S1156 Synonyms: RO 09-1978
Molecular Weight(MW): 359.35
Capecitabine is a tumor-selective fluoropyrimidine carbamate, which achieves higher intratumoral 5-FU level with lower toxicity than 5-FU.
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2. For more details, such as half maximal inhibitory concentrations (IC50s) and working concentrations of each inhibitor, please click on the link of the inhibitor of interest.
3. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation.
4. Orange "√" refers to compounds which do inhibitory effects on the related isoform, but without specific value.
|Description||Capecitabine is a tumor-selective fluoropyrimidine carbamate, which achieves higher intratumoral 5-FU level with lower toxicity than 5-FU.|
|Features||A tumor-selective fluoropyrimidine carbamate.|
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. 
|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.  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. |
|In vitro||DMSO||72 mg/mL (200.36 mM)|
|Ethanol||72 mg/mL (200.36 mM)|
|Water||6 mg/mL (16.69 mM)|
* 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.
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Clinical Trial Information
|NCT Number||Recruitment||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT02393755||Recruiting||Colon Adenocarcinoma|Rectal Adenocarcinoma|Recurrent Colon Carcinoma|Recurrent Rectal Carcinoma|Stage IVA Colon Cancer|Stage IVA Rectal Cancer|Stage IVB Colon Cancer|Stage IVB Rectal Cancer||Roswell Park Cancer Institute|National Cancer Institute (NCI)|Boehringer Ingelheim|National Comprehensive Cancer Network||May 8, 2015||Phase 1|Phase 2|
|NCT02352831||Recruiting||Pancreatic Cancer|Cancer of Pancreas|Cancer of the Pancreas|Pancreas Cancer||Washington University School of Medicine||August 31, 2015||Phase 1|Phase 2|
|NCT03050814||Not yet recruiting||Colorectal Cancer||National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC)||February 3, 2017||Phase 2|
|NCT01497392||Completed||Adenocarcinoma of the Pancreas|Stage III Pancreatic Cancer|Stage IV Pancreatic Cancer|Unspecified Adult Solid Tumor, Protocol Specific||Roswell Park Cancer Institute|National Cancer Institute (NCI)|Novartis||March 29, 2012||Phase 1|
|NCT01134601||Terminated||Non-Metastatic Adenocarcinoma of the Rectum||National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC)||May 24, 2010||Phase 1|
|NCT02954055||Not yet recruiting||Breast Cancer||International Breast Cancer Study Group||May 2017||Phase 2|
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