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MedChemExpress - Model Trifluridine - ...

MedChemExpress - Model Trifluridine - 70-00-8

Trifluridine (Trifluorothymidine) is an irreversible and orally active thymidylate synthase inhibitor, and thereby suppressing DNA synthesis. Trifluridine is an antiviral molecule used for research of HSV, rhabdovirus and orthopoxvirus infection. Trifluridine induces cell apoptosis and autophagy. Trifluridine is also an anticancer agent used in studies of metastatic colorectal cancer, gastrointestinal tumors[1][2][3][4].

Trifluridine

MCE China：Trifluridine

Brand：MedChemExpress (MCE)

Cat. No.HY-A0061

CAS：70-00-8

Synonyms：Trifluorothymidine; 5-Trifluorothymidine; TFT

Purity：99.83%

Storage：Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year

Shipping：Room temperature in continental US; may vary elsewhere.

Description：Trifluridine (Trifluorothymidine) is an irreversible and orally active thymidylate synthase inhibitor, and thereby suppressing DNA synthesis. Trifluridine is an antiviral molecule used for research of HSV, rhabdovirus and orthopoxvirus infection. Trifluridine induces cell apoptosis and autophagy. Trifluridine is also an anticancer agent used in studies of metastatic colorectal cancer, gastrointestinal tumors.

In Vitro：Trifluridine (0.5 μΜ, 3 days) induces cellular senescence in HUVECs[2]. Trifluridine (0.5 μΜ, 3 days) inhibits autophagy and autophagy flux via the mTOR pathway in HUVECs [2]. Trifluridine (0-5 μΜ, 3 days) inhibits HUVEC cells viability in a concentration-dependent way[2]. Trifluridine (5 µM-20 µM, 24 h–72 h) inhibits the proliferation in MCF-7, MDA-MB-231, BT-549 and Hs578T[4]. Trifluridine (0 µM-20 µM, 48 h) selectively induces apoptosis in MCF-7, MDA-MB-231, BT-549 and Hs578T cells [4]. Trifluridine (10 µM, 72 h) induces DNA double-strand break in MCF-10A, MCF-7, MDA-MB-231 and BT-549 cells[4].

In Vivo：Trifluridine/tipiracil (200 mg/kg, PO, twice daily for 5 consecutive days followed by 2 drug-free days for 6 weeks) shows antitumor activity in the human colorectal intraperitoneal xenograft model[3]. Trifluridine (75 or 150 mg/kg, oral gavage, once daily for 5 consecutive days) inhibits the growth in implanted mouse TNBC tumors [4].

IC50 & Target：Thymidylate Synthase Nucleoside Antimetabolite/Analog HSV-1 HSV-2

References：

[1]. Okayama T, et al. Involvement of concentrative nucleoside transporter 1 in intestinal absorption of trifluorothymidine, a novel antitumor nucleoside, in rats. J Pharmacol Exp Ther. 2012 Feb;340(2):457-62. [Content Brief]

[2]. Jia HJ, et al. Trifluridine induces HUVECs senescence by inhibiting mTOR-dependent autophagy. Biochem Biophys Res Commun. 2022 Jun 25;610:119-126. [Content Brief]

[3]. Suzuki N,et al. Trifluridine/tipiracil increases survival rates in peritoneal dissemination mouse models of human colorectal and gastric cancer. Oncol Lett. 2017 Jul;14(1):639-646. [Content Brief]

[4]. Li J, et al. Trifluridine selectively inhibits cell growth and induces cell apoptosis of triple-negative breast cancer. Am J Cancer Res. 2020 Feb 1;10(2):507-522. [Content Brief]

Brand introduction:
•   MCE (MedChemExpress) has a global exclusive compound library of more than 200 kinds, and we are committed to providing the most comprehensive range of high-quality small molecule active compounds for scientific research customers around the world；
•   More than 50,000 highly selective inhibitors and agonists are involved in various popular signaling pathways and disease areas；
•   The products cover a variety of recombinant proteins, peptides, commonly used kits, more PROTAC, ADC and other characteristic products, widely used in new drug research and development, life science and other scientific research projects；
•   Provide virtual screening, ion channel screening, metabolomics analysis detection analysis, drug screening and other professional technical services；
•   It has a professional experimental center and strict quality control and verification system；
•   Provide LC/MS, NMR, HPLC, chiral analysis, elemental analysis and other quality inspection reports to ensure the high purity and high quality of products；
•   The biological activity of the products has been verified by the experiments of customers in various countries；
•   A variety of top journals such as Nature, Cell, Science and pharmaceutical patents have included the scientific research results of MCE customers；
•   Our professional team tracks the latest pharmaceutical and life science research and provides you with the latest active compounds in the world；
•   It has established long-term cooperation with the world's major pharmaceutical companies and well-known scientific research institutions。