Carmofur

This product is for research use only, not for human use. We do not sell to patients.

Carmofur
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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
Molecular FormulaC11H16FN3O3
CAS No.61422-45-5
Storage-20℃ for 3 years in powder formr
-80℃ for 2 years in solvent
Solubility In VitroDMSO: 52 mg/mL (202.1 mM)r
Water: <1 mg/mLr
Ethanol: 10 mg/mL (38.9 mM)
SMILES CodeO=C(N(C(N1)=O)C=C(F)C1=O)NCCCCCC
SynonymsHCFU; 1-hexylcarbamoyl-5-fluorouracil
ProtocolIn VitroIn 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.
In VivoCarmofur 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 modelNude mice
These protocols are for reference only. InvivoChem does not independently validate these methods.
Preparing Stock Solutions
Solvent volume to be added Mass (the weight of a compound)
Mother liquor concentration 1mg5mg10mg20mg
1mM3.8871 mL19.4356 mL38.8712 mL77.7424 mL
5mM0.7774 mL3.8871 mL7.7742 mL15.5485 mL
10mM0.3887 mL1.9436 mL3.8871 mL7.7742 mL
20mM0.1944 mL0.9718 mL1.9436 mL3.8871 mL
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%DMSO + % + %Tween 80 + %ddH2O

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Method for preparing DMSO master liquid: mg drug pre-dissolved in µL DMSO(Master liquid concentration mg/mL) ,Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation: Take µL DMSO master liquid, next add µL PEG300, mix and clarify, next add µL Tween 80,mix and clarify, next add µL ddH2O,mix and clarify.
Note:
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