Trifluridine

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

三氟胸苷 (TFT) 是胸苷磷酸化酶的抑制剂。

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