TAS-102 is an orally administered combination of trifluridine and Tipiracil hydrochloride in a molar ratio of 1:0.5. Trifluridine is the active antitumor component of TAS-102; its monophosphate form inhibits thymidylate synthase, and its triphosphate form is incorporated into DNA in tumor cells.
In vivo, TAS-102 monotherapy has a significant antitumor activity against KM12C/5-FUFU-bearing nude mice. TAS-102 can overcome acquired resistance to 5-FU because the main mechanism of TAS-102 is not associated with main metabolic enzymes of 5-FU, such as TS and OPRT. TAS-102 has demonstrated efficacy in 5-FU-refractory cancers.
|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: ≥ 10 mg/mL warmed|
TAS-102: a novel antimetabolite for the 21st century.
Uboha N, et al. Future Oncol. 2016 Jan;12(2):153-63. PMID: 26616466.
TAS-102, a novel antitumor agent: a review of the mechanism of action.
Lenz HJ, et al. Cancer Treat Rev. 2015 Nov;41(9):777-83. PMID: 26428513.
Exposure-dependent incorporation of trifluridine into DNA of tumors and white blood cells in tumor-bearing mouse.
Yamashita F, et al. Cancer Chemother Pharmacol. 2015 Aug;76(2):325-33. PMID: 26084259.
Efficacy of combination chemotherapy using a novel oral chemotherapeutic agent, TAS-102, with irinotecan hydrochloride on human colorectal and gastric cancer xenografts.
Nukatsuka M, et al. Anticancer Res. 2015 Mar;35(3):1437-45. PMID: 25750295.
|Related DNA/RNA Synthesis Products|
Chebulinic acid is a potent natural inhibitor of M. tuberculosis DNA gyrase, also can inhibit SMAD-3 phosphorylation, inhibit H+ K+-ATPase activity.
Brivudine is a uridine derivative and nucleoside analog with pro-apoptotic and chemosensitizing properties. It is incorporated into the viral DNA and blocks the action of DNA polymerases, thus inhibiting viral replication.
5-methoxyflavone is a novel DNA polymerase-beta inhibitor and neuroprotective agent against beta-amyloid toxicity.
5-BrdU is a synthetic thymidine analog; used for cell proliferation assays.
Madrasin is a potent and cell penetrant splicing inhibitor that interferes with the early stages of spliceosome assembly.
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2017 AbMole BioScience. All Rights Reserved.