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.
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
|Source||Cancer Biol Ther (2018). Figure 6. 5-FU (Abmole Bioscience, Shanghai, China)|
|Method||Buformin synergizes with chemotherapy|
|Cell Lines||C33A cells|
|Results||In C33A cells, low-dose buformin (1μM) significantly enhanced the anti-proliferative effects when combined with cisplatin, paclitaxel, or 5-FU|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.
|Solubility||DMSO 20 mg/mL (Need ultrasonic and warming)|
Amphiphilic dendritic nanomicelle-mediated co-delivery of 5-fluorouracil and doxorubicin for enhanced therapeutic efficacy.
Han R, et al. J Drug Target. 2017 Feb;25(2):140-148. PMID: 27356094.
Gastrointestinal dysfunction and enteric neurotoxicity following treatment with anticancer chemotherapeutic agent 5-fluorouracil.
McQuade RM, et al. Neurogastroenterol Motil. 2016 Dec;28(12):1861-1875. PMID: 27353132.
Knockdown of NFBD1/MDC1 enhances chemosensitivity to cisplatin or 5-fluorouracil in nasopharyngeal carcinoma CNE1 cells.
Zeng Q, et al. Mol Cell Biochem. 2016 Jul;418(1-2):137-46. PMID: 27334757.
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Chebulinic acid is a potent natural inhibitor of M. tuberculosis DNA gyrase, also can inhibit SMAD-3 phosphorylation, inhibit H+ K+-ATPase activity.
TAS-102 is an orally administered combination of a thymidine-based nucleic acid analogue, trifluridine, and a thymidine phosphorylase inhibitor, tipiracil hydrochloride.
6-Thio-2′-deoxyguanosine (6-thio-dG) is a nucleoside analog and telomerase substrate that is incorporated into de novo–synthesized telomeres.
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