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Size | Price | Stock |
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2g | $180 | Check With Us |
5g | $299 | Check With Us |
10g | $445 | Check With Us |
Cat #: V0019 CAS #: 61422-45-5 Purity ≥ 99%
Description: Carmofur (also known as HCFU), a derivative of fluorouracil (5-FU) which is an antimetabolite class of anticancer drug, is a novel, highly potent acid ceramidase inhibitor used in the treatment of breast and colorectal cancer. Carmofur is one of the masked compounds (a sort of prodrug) of 5-FU, which was modified to achieve more potent antineoplastic activity and less side effects. 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: [1]. Realini N, et al. Discovery of highly potent acid ceramidase inhibitors with in vitro tumor chemosensitizing activity. Sci Rep. 2013;3:1035.
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Molecular Weight (MW) | 257.26 |
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Molecular Formula | C11H16FN3O3 |
CAS No. | 61422-45-5 |
Storage | -20℃ for 3 years in powder formr |
-80℃ for 2 years in solvent | |
Solubility In Vitro | DMSO: 52 mg/mL (202.1 mM)r |
Water: <1 mg/mLr | |
Ethanol: 10 mg/mL (38.9 mM) | |
SMILES Code | O=C(N(C(N1)=O)C=C(F)C1=O)NCCCCCC |
Synonyms | HCFU; 1-hexylcarbamoyl-5-fluorouracil |
Protocol | 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. Cell Assay: Carmofur is a derivative of fluorouracil, an antimetabolite used as an antineoplastic agent. Target: Nucleoside antimetabolite/analog Carmofur, which is used in the clinic to treat colorectal cancers, is a potent AC inhibitor and that this property is essential to its anti-proliferative effects. Carmofur inhibited AC activity with a median effective concentration (IC50) of 29 ± 5 nM (mean ± standard error of the mean, s.e.m.; n = 4), whereas 5-FU had no such effect (IC50>1 mM). systemic administration of carmofur (10 or 30 mg-kg-1, intraperitoneal, i.p.) to mice produced a dose-dependent inhibition of AC activity in various tissues, including lungs and brain cortex. |
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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 | Nude mice |
Solvent volume to be added | Mass (the weight of a compound) | |||
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Mother liquor concentration | 1mg | 5mg | 10mg | 20mg |
1mM | 3.8871 mL | 19.4356 mL | 38.8712 mL | 77.7424 mL |
5mM | 0.7774 mL | 3.8871 mL | 7.7742 mL | 15.5485 mL |
10mM | 0.3887 mL | 1.9436 mL | 3.8871 mL | 7.7742 mL |
20mM | 0.1944 mL | 0.9718 mL | 1.9436 mL | 3.8871 mL |
This equation is commonly abbreviated as: C1 V1 = C2 V2
- (1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
- (2) Be sure to add the solvent(s) in order.