5-fluorouracil (5-FU) is a chemotherapy compound that is a pyrimidine analog which is used in the treatment of cancer. 5-fluorouracil (5-FU) works through noncompetitive inhibition of thymidylate synthase. Fluorouracil IC50 values were observed across the National Cancer Institute NCI60 panel of human tumor cell lines, which exhibit a mean IC50 of 17.6 μM, with a range of 1~501 μM.
In vivo, 5-fluorouracil (23 mg/kg, 3 times/week) for 14 days, induces accelerated gastrointestinal transit associated with acute intestinal inflammation at day 3 after the start of treatment, which may have led to persistent changes in the ENS observed after days 7 and 14 of treatment contributing to delayed gastrointestinal transit and colonic dysmotility.
Molecules. 2023 Apr 10;28(8), 3351.
The Large Molecular Weight Polysaccharide from Wild Cordyceps and Its Antitumor Activity on H22 Tumor-Bearing Mice
5-fluorouracil purchased from AbMole
Drυg Discοv Ther. 2020 Sep 8;14(4):197-203.
MicroRNA analysis of NCI-60 human cancer cells indicates that miR-720 and miR-887 are potential therapeutic biomarkers for breast cancer
5-fluorouracil purchased from AbMole
Cancer Biol Ther. 2018 Feb 5.
Buformin suppresses proliferation and invasion via AMPK/S6 pathway in cervical cancer and synergizes with paclitaxel
5-fluorouracil purchased from AbMole
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Source | Drug Discoveries & Therapeutics 2020. Figure 4. 5-Fu (Abmole Bioscience Inc, Houston, TX, USA) |
| Method | MTT assay | |
| Cell Lines | A549, H460, H322M, MCF-7, T47-D and MDA-MB-231 cells | |
| Concentrations | - | |
| Incubation Time | 72 h | |
| Results | The current study verified that the anti-cancer effect of perifosine was significantly enhanced by inhibiting miR-720 and that the anti-cancer effect of 5-Fu was significantly enhanced by inhibiting miR-887 in breast cancer cells |
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Source | Cancer Biol Ther (2018). Figure 6. 5-FU (Abmole Bioscience, Shanghai, China) |
| Method | Buformin synergizes with chemotherapy | |
| Cell Lines | C33A cells | |
| Concentrations | 1 μM | |
| Incubation Time | ||
| Results | In C33A cells, low-dose buformin (1μM) significantly enhanced the anti-proliferative effects when combined with cisplatin, paclitaxel, or 5-FU |
| Molecular Weight | 130.08 |
| Formula | C4H3FN2O2 |
| CAS Number | 51-21-8 |
| Solubility (25°C) | DMSO ≥ 25 mg/mL Water ≥ 5 mg/mL |
| Storage | 4°C, protect from light, dry, sealed |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
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