Trifluridine

Research use only, not for human use.

Trifluorothymidine (TFT) and is an inhibitor of thymidine phosphorylase.

Trifluorothymidine (TFT) and is an inhibitor of thymidine phosphorylase. TFT also inhibits thymidylate synthase (TS), a rate-limiting enzyme of DNA biosynthesis, and is incorporated into DNA.

Cell Viability Assay Cell Line:HUVEC cellsConcentration: 0-5 μM Incubation Time:3 days Result:Cell viability dropped sharply at 3 μM and 5 μM.Immunofluorescence Cell Line:HUVEC cells Concentration: 0-5 μM Incubation Time:3 days Result:Induced cellular senescence by inhibiting autophagy flux.Western Blot Analysis Cell Line:HUVEC cells Concentration: 0-5 μM Incubation Time:3 daysResult:Increased protein levels of senescence markers: p53, p16, SASP (IL-1, IL-6, TNF-α, p21).Cell Proliferation AssayCell Line:MCF-7, MDA-MB-231, BT-549, Hs578T and MCF-10A(control non-tumor) cells Concentration:5 μM-20 μM Incubation Time:24 h–72 h Result:Inhibited the proliferation of MDA-MB231, BT549 and Hs578T cells at 10μM and 20μM, significantly.Apoptosis AnalysisCell Line: MDA-MB-231, BT-549, and Hs578T cells Concentration:10μM or 20 μMIncubation Time:48 h Result:Increased the percentages of apoptotic TNBC cells (MDA-MB-231, BT-549, and Hs578Tcells) at 10μM and 20μM, significantly.

Animal Model:Nude mice (human colorectal intraperitoneal xenograft model) Dosage: 200 mg/kg(trifluridine/tipiracil)Administration:Oral administration; Once a day; 5 days followed by 2 drug-free days, a total of 6 weeks Result:Exhibited a significantly longer survival time compared with untreated mice.Animal Model:Mouse model of breast cancerDosage:75 or 150 mg/kg Administration:Oral gavage; daily for 10 days Result:Treatment with different doses inhibited the growth of TNBC tumors in mouse in a dose-dependent mannerAnimal Model:The human gastric MKN45 intraperitoneal xenograft model Dosage:200 mg/kg (Trifluridine/tipiracil)Administration:twice daily for 5 consecutive days followed by 2 drug?free days for 6 weeks Result:Prolonged the survival of mice compared with untreated mice.

NSC 75520 | NSC 529182 | TFT | Trifluridine

Cell Cycle/DNA Damage

DNA/RNA Synthesis

DNA/RNA Synthesis| Thymidylate synthase

Cancer

——

70-00-8

296.2

C10H11F3N2O5

>98% (HPLC)

Ethanol: 59 mg/mL (199.18 mM); Water: 59 mg/mL (199.18 mM); DMSO: 59 mg/mL (199.18 mM)

O=C1NC(C(C(F)(F)F)=CN1[C@@H]2O[C@H](CO)[C@@H](O)C2)=O

1-((2R,4S,5R)-4-hydroxy-5-(hydroxymethyl)tetrahydrofuran-2-yl)-5-(trifluoromethyl)pyrimidine-2,4(1H,3H)-dione.

(-20℃)

With Ice Pack

≥ 2 years