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| 100mg |
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| 250mg |
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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.
| ln Vitro |
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.
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| ln Vivo |
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| 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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| Animal Protocol |
Nude mice
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| References | ||
| Additional Infomation |
Carmofur is an organohalogen compound and a member of pyrimidines.
Carmofur is a derivative of fluorouracil, and is an antineoplastic agent that has been used in the treatment of breast and colorectal cancer. Carmofur has been known to induce leukoencephalopathy. Carmofur is an antimetabolite (pyrimidine analogue) antineoplastic derivative of 5-fluorouracil. (NCI) |
| Molecular Formula |
C11H16FN3O3
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| Molecular Weight |
257.26
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| Exact Mass |
257.117
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| Elemental Analysis |
C, 51.36; H, 6.27; F, 7.38; N, 16.33; O, 18.66
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| CAS # |
61422-45-5
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| Related CAS # |
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| PubChem CID |
2577
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| Appearance |
White to off-white solid powder
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| Density |
1.3±0.1 g/cm3
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| Melting Point |
110-111
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| Index of Refraction |
1.525
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| LogP |
2.58
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
18
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| Complexity |
382
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| Defined Atom Stereocenter Count |
0
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| SMILES |
FC1C(N([H])C(N(C=1[H])C(N([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])[H])=O)=O)=O
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| InChi Key |
AOCCBINRVIKJHY-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C11H16FN3O3/c1-2-3-4-5-6-13-10(17)15-7-8(12)9(16)14-11(15)18/h7H,2-6H2,1H3,(H,13,17)(H,14,16,18)
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| Chemical Name |
5-fluoro-N-hexyl-2,4-dioxo-3,4-dihydropyrimidine-1(2H)-carboxamide
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| Synonyms |
HCFU; 1hexylcarbamoyl5fluorouracil;
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: 2.08 mg/mL (8.09 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (8.09 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (8.09 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.8871 mL | 19.4356 mL | 38.8712 mL | |
| 5 mM | 0.7774 mL | 3.8871 mL | 7.7742 mL | |
| 10 mM | 0.3887 mL | 1.9436 mL | 3.8871 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(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.
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