Tegafur-gimeracil-oteracil potassium  (Synonyms: S-1; TS-1)

Tegafur-gimeracil-oteracil potassium (S-1; TS-1) is an orally active anticancer agent composed of Tegafur (HY-17400), Gimeracil (HY-17469), and Oteracil potassium (HY-17511). Tegafur-gimeracil-oteracil potassium inhibits the proliferation, migration and invasion of endometrial cancer cells and induces apoptosis by blocking the PI3K/AKT/mTOR signaling pathway. Tegafur-gimeracil-oteracil potassium can be used in research related to endometrial cancer and gastric cancer with peritoneal metastasis^[1][2].

Tegafur-gimeracil-oteracil potassium (1-50 μg/mL; 6-48 h) significantly inhibits the viability of Ishikawa and HEC-1-A endometrial cancer cells in a dose- and time-dependent manner, with corresponding IC₅₀ values of 16.26 μg/mL and 11.33 μg/mL for the two cell lines, respectively^[1].
Tegafur-gimeracil-oteracil potassium (5-50 μg/mL; 24-72 h) inhibits the proliferation of Ishikawa and HEC-1-A endometrial cancer cells in a concentration-dependent manner^[1].
Tegafur-gimeracil-oteracil potassium (5-50 μg/mL) reduces DNA synthesis capacity and proliferative activity of Ishikawa and HEC-1-A endometrial cancer cells in a concentration-dependent manner^[1].
Tegafur-gimeracil-oteracil potassium (5-50 μg/mL; 24 h) inhibits the migration of Ishikawa and HEC-1-A endometrial cancer cells in a dose-dependent manner^[1].
Tegafur-gimeracil-oteracil potassium (5-50 μg/mL; 24 h) inhibits the invasion of Ishikawa and HEC-1-A endometrial cancer cells in a dose-dependent manner^[1].
Tegafur-gimeracil-oteracil potassium (5-50 μg/mL) promotes apoptosis of Ishikawa and HEC-1-A endometrial cancer cells in a concentration-dependent manner^[1].
Tegafur-gimeracil-oteracil potassium (10-25 μg/mL) upregulates the mRNA expression of the pro-apoptotic protein Bax and downregulates the mRNA expression of the anti-apoptotic protein Bcl-2 in Ishikawa and HEC-1-A endometrial cancer cells^[1].
Tegafur-gimeracil-oteracil potassium (10-25 μg/mL) upregulates the expression of the pro-apoptotic Bax protein and downregulates the expression of the anti-apoptotic Bcl-2 protein in Ishikawa and HEC-1-A endometrial cancer cells^[1].
Tegafur-gimeracil-oteracil potassium (25 μg/mL) inhibits the PI3K/AKT/mTOR signaling pathway by reducing the phosphorylation levels of PI3K, AKT and mTOR in Ishikawa and HEC-1-A endometrial cancer cells^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

540.89

C₁₇H₁₅ClFKN₆O₉

150863-82-4

Solid

White to off-white

O=C(C1=NC(NC(N1)=O)=O)O[K].O=C2C=C(C(Cl)=CN2)O.O=C3NC(N(C4OCCC4)C=C3F)=O

Room temperature in continental US; may vary elsewhere.

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

• [1]. Si Y, et al. TS-1 inhibits endometrial cancer cell proliferation, migration, and apoptosis by blocking the PI3K/AKT/mTOR signaling pathway. Am J Transl Res. 2025;17(10):8312-8323. Published 2025 Oct 25.  [Content Brief]

  [2]. Osugi H, et al. Oral fluoropyrimidine anticancer drug TS-1 for gastric cancer patients with peritoneal dissemination. Oncol Rep. 2002;9(4):811-815.  [Content Brief]