product name Carmofur
Description: Carmofur (also known as HCFU) is a highly potent acid ceramidase inhibitor used in the treatment of breast and colorectal cancer. Carmofur is one of the masked compounds of 5-FU, which was modified for more potent antineoplastic activity and less toxicity. Carmofur is converted in vivo into 5-FU directly or via intermetabolites, such as 1-(carboxypentylcarbamoyl)-5-fluorouracil and/or 1-(carboxypropylcarbomoyl)-5-fluorouraci. Carmofur and its metabolites gradually accumulate in the brain during continuous administration and are removed very slowly.
References: J Neurol. 1987 Aug;234(6):365-70; Acta Neuropathol. 1996 Jul;92(1):8-13.
257.26
Formula
C11H16FN3O3
CAS No.
61422-45-5
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 52 mg/mL (202.1 mM)
Water: <1 mg/mL
Ethanol: 10 mg/mL (38.9 mM)
Solubility (In vivo)
Synonyms
HCFU
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19412328
| In Vitro |
In vitro activity: Carmofur is one of the masked compounds of 5-FU, which was modified for more potent antineoplastic activity and less toxicity. Carmofur is converted in vivo into 5-FU directly or via intermetabolites, such as 1-(carboxypentylcarbamoyl)-5-fluorouracil and/or 1-(carboxypropylcarbomoyl)-5-fluorouraci. Carmofur and its metabolites gradually accumulate in the brain during continuous administration and are removed very slowly. Carmofur has potent neurotoxicity which can produce severe leucoencephalopathy resembling methotrexate leucoencephalopathy both clinically and on brain CT, together with a cerebellar syndrome similar to that following 5-FU neurotoxicity. Kinase Assay: Cell Assay: |
|---|---|
| In Vivo | Carmofur or 5-FU together with Nicardipine, a Ca2+ antagonist, causes a higher level of the FU in tumor tissue and potentiation of an antitumor effect on human gastric cancer transplanted into nude mice. Carmofur exerts almost the same growth-inhibitory effects on both tumors in therapeutic experiments using nude mice bearing parent or subcutaneously transplanted 5-FU-resistant DLD-1 cells. |
| Animal model | |
| Formulation & Dosage | |
| References | J Neurol. 1987 Aug;234(6):365-70; Acta Neuropathol. 1996 Jul;92(1):8-13. |
