Trifluridine

SKU: orb1224196

Description

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.

Key Properties

• CAS Number: 70-00-8
• MW: 296.2
• Purity: >98% (HPLC)
• Formula: C₁₀H₁₁F₃N₂O₅
• SMILES: O=C1NC(C(C(F)(F)F)=CN1[C@@H]2O[C@H](CO)[C@@H](O)C2)=O
• Target: DNA/RNA Synthesis
• Solubility: Ethanol: 59 mg/mL (199.18 mM); Water: 59 mg/mL (199.18 mM); DMSO: 59 mg/mL (199.18 mM)

Bioactivity

• In Vivo:
  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 cancer. Dosage: 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 manner. Animal 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.
• In Vitro:
  Cell Viability Assay Cell line: HUVEC cells. Concentration: 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 days. Result: Increased protein levels of senescence markers: p53, p16, SASP (IL-1, IL-6, TNF-α, p21). Cell Proliferation Assay Cell 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 10 μM and 20 μM, significantly. Apoptosis Analysis Cell line: MDA-MB-231, BT-549, and Hs578T cells. Concentration: 10 μM or 20 μM. Incubation time: 48 h. Result: Increased the percentages of apoptotic TNBC cells (MDA-MB-231, BT-549, and Hs578Tcells) at 10 μM and 20 μM, significantly.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

NSC 75520 | NSC 529182 | TFT | Trifluridine

Quick Database Links

Gene Symbol

DNA/RNA Synthesis