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|
BMVC-8C3O is a DNA G-quadruplexe (G4) ligand which can induce topological conversion of non-parallel to parallel forms in human telomeric DNA G4s.
TH5487 is a selective 8-oxoguanine DNA glycosylase 1 (OGG1) inhibitor with an IC50 of 342 nM.
COH29 is an orally available, aromatically substituted thiazole and inhibitor of the human ribonucleotide reductase (RNR), with potential antineoplastic activity.
Plicamycin, also known as mithramycin or Mithramycin A is a n antibiotic isolated from the bacterium Streptomyces plicatus with antineoplastic activity.
GC7 Sulfate is a deoxyhypusine synthase (DHPS) inhibitor.
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2020 AbMole BioScience. All Rights Reserved.