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TAS-102

Cat. No. M9020
TAS-102 Structure
Synonym:

Trifluridine/Tipiracil HCl; Trifluridine-tipiracil hydrochloride mixture

Size Price Availability Quantity
5mg USD 100 In stock
25mg USD 300 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

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.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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 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.

Chemical Information
Molecular Weight 575.32
Formula C19H23Cl2F3N6O7
CAS Number 733030-01-8
Purity >99%
Solubility DMSO: ≥ 10 mg/mL warmed
Storage at -20°C
References

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.

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Keywords: TAS-102, Trifluridine/Tipiracil HCl; Trifluridine-tipiracil hydrochloride mixture supplier, DNA/RNA Synthesis, inhibitors

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