Carmofur

Cytostatic derivative of fluorouracilm,antineoplatic agent CAS# 61422-45-5

Carmofur

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Carmofur

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Chemical Properties of Carmofur

Cas No. 61422-45-5 SDF Download SDF
PubChem ID 2577 Appearance Powder
Formula C11H16FN3O3 M.Wt 257.26
Type of Compound N/A Storage Desiccate at -20°C
Solubility DMSO : ≥ 100 mg/mL (388.71 mM)
H2O : < 0.1 mg/mL (insoluble)
*"≥" means soluble, but saturation unknown.
Chemical Name 5-fluoro-N-hexyl-2,4-dioxopyrimidine-1-carboxamide
SMILES CCCCCCNC(=O)N1C=C(C(=O)NC1=O)F
Standard InChIKey AOCCBINRVIKJHY-UHFFFAOYSA-N
Standard InChI 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)
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Carmofur Dilution Calculator

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Carmofur Molarity Calculator

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Preparing Stock Solutions of Carmofur

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 3.8871 mL 19.4356 mL 38.8712 mL 77.7424 mL 97.178 mL
5 mM 0.7774 mL 3.8871 mL 7.7742 mL 15.5485 mL 19.4356 mL
10 mM 0.3887 mL 1.9436 mL 3.8871 mL 7.7742 mL 9.7178 mL
50 mM 0.0777 mL 0.3887 mL 0.7774 mL 1.5548 mL 1.9436 mL
100 mM 0.0389 mL 0.1944 mL 0.3887 mL 0.7774 mL 0.9718 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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Background on Carmofur

Carmofur is a cytostatic derivative of fluorouracil.

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References on Carmofur

[Neo-adjuvant chemotherapy with carmofur for colorectal cancer--a multi-institutional randomized controlled study].[Pubmed:12465390]

Gan To Kagaku Ryoho. 2002 Nov;29(11):1917-24.

The efficacy and safety of preoperative chemotherapy with Carmofur (HCFU) for colorectal cancer were evaluated in a randomized controlled study involving 63 institutes in the Kanto area. Patients aged 75 or younger with Dukes' B or C colorectal cancer were eligible if curative surgery was expected. In the end, 326 were eligible from 405 consecutive colorectal cancer patients. Patients in both the control (n = 162) and the new treatment group (n = 164) were given intravenous mitomycin C (MMC) 6 mg/m2 on day 0 and 7 after surgery and HCFU 300 mg/day orally from day 14 for a year. Patients in the new treatment group were also given oral HCFU for 14 days or more prior to surgery. All 326 patients were followed for 5 years or longer. Five-year overall and disease-free survival rates were not significantly different between the two groups (75.4% and 71.6% for the control, and 71.8% and 71.5% for the study group, respectively). In the subset analysis, neither cancer site nor nodal status affected the differences in overall- and disease-free survival rates between the groups. The present findings show no additional efficacy of preoperative chemotherapy with HCFU in survival from advanced colorectal cancer. Further investigations in terms of patient selection, treatment regimen, combined use of radiotherapy, and other factors would be required to determine the significance of preoperative chemotherapy against advanced colorectal cancer.

Anti-tumor activity of carmofur water-solubilized by lactic acid oligomer-grafted pullulan nanogels.[Pubmed:19928152]

J Nanosci Nanotechnol. 2009 Aug;9(8):4797-804.

Nanogels of pullulan grafted with L-lactic acid oligomer (LLA-o) were prepared to allow a lipophilic anti-tumor drug, Carmofur, to solubilize in water. The number of LLA-o grafted was increased with an increase in the amount of LLA-o added in preparation. The LLA-o-grafted pullulan showed critical aggregation concentrations and had 20-100 nm in diameter depending on the grafted number. The Carmofur was water-solubilized by the LLA-o-grafted pullulan self-assemble (nanogel), and inhibited the in vitro growth of tumor cells to a similar or high extent compared with Carmofur solution in dimethyl sulfoxide (DMSO). When incubated with the spheroid of tumor cells, the nanogel with Carmofur showed a strong suppressive effect of tumor cells grown, in contrast to the Carmofur solution. When intratumorally injected into mice carrying a tumor mass, Carmofur water-solubilized by the nanogel showed stronger suppressive effect of tumor cells growth. It is concluded that the nanogel is a promising carrier to water-solubilize Carmofur and enhance the in vitro and in vivo anti-tumor effects.

Postoperative adjuvant use of carmofur for early breast cancer.[Pubmed:15179836]

Osaka City Med J. 2003 Dec;49(2):77-83.

OBJECTIVE: The efficacy of oral fluoropyrimidine Carmofur was evaluated for adjuvant use for breast cancer. METHODS: 150 patients with breast cancer of T0N1, T1, N1, T2N0, and T2N1 were randomized to 100 for Carmofur and 50 for carboquone. Both drugs were administered continuously for 28 days cyclically for 5 years with a cessation period of 28 days for Carmofur and 56 days for carboquone. RESULTS: Overall survival excluding non-breast cancer death was 90% for the Carmofur group and 88% for the carboquone group, adjusted by Cox's regression analysis. Difference in drug never affected survival. Leukocyte count was decreased in the carboquone group, but no change in serum transaminase was found in either group. Ten patients, 5 for Carmofur and 5 for carboquone, suffered from second malignancy, more than expected in the normal population, but difference in the cumulative rate of each group was not significant. CONCLUSION: Adjuvant use of Carmofur as well as carboquone is beneficial for early breast cancer.

An individual patient data meta-analysis of adjuvant therapy with carmofur in patients with curatively resected colon cancer.[Pubmed:16155120]

Jpn J Clin Oncol. 2005 Sep;35(9):536-44.

BACKGROUND: Oral Carmofur, either as a single or in combination with other chemotherapeutic agents, has been used as adjuvant chemotherapy for curatively resected colon cancer patients. Past trials and meta-analyses indicate that it is somewhat effective in extending survival of patients with this cancer. The objective of this study was to perform a reappraisal of randomized clinical trials conducted in this regard. METHODS: We designed an individual patient-based meta-analysis of relevant clinical trials to examine the benefit of oral Carmofur for curatively resected colon cancer in terms of overall survival (OS) and disease-free survival (DFS). RESULTS: We analyzed individual patient data of three randomized clinical trials, which met the predetermined inclusion criteria. These three trials had a combined total of 2152 patients, Carmofur as adjuvant chemotherapy compared with surgery-alone, 5 years follow-up, intention-to-treat-based analytic strategy and similar end points (OS and DFS). In a pooled analysis, 5 year OS rates were 80.4 and 76.4%, and 5 year DFS rates 76.9 and 71.0%, respectively, in Carmofur and surgery-alone group. Oral Carmofur had significant advantage over surgery-alone in terms of both OS [pooled hazard ratio, 0.82; 95% confidence interval (CI) = 0.68-0.99; P = 0.043] and DFS (pooled hazard ratio, 0.77; 95% CI = 0.65-0.91; P = 0.003). CONCLUSIONS: This individual patient-based meta-analysis demonstrated that oral Carmofur significantly improves both OS and DFS in patients with curatively resected colon cancers.

Description

Carmofur is a derivative of fluorouracil, an antimetabolite used as an antineoplastic agent.

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