TVB-3166

SKU: orb1940685

Description

TVB-3166 induces apoptosis and inhibits in-vivo xenograft tumor growth. TVB-3166 is a reversible and selective fatty acid synthase inhibitor (IC50s: 42 nM and 81 nM for biochemical FASN and cellular palmitate synthesis, respectively).(In Vitro):TVB-3166 (0.2 μM; 48 hours) inhibits β-catenin pathway signal transduction and transcriptional activity. TVB-3166 (0.02 or 0.20 μM; 7 days) suppresses palmitate synthesis and tumor cell viability in a dose-dependent manner. TVB-3166 (0.001-10 μM; 24 hours) induces cell death in CALU-6 non-small-cell lung tumor cells (cellular IC50: 0.10 μM) . (In Vivo):TVB-3166 (Oral gavage; 30-100 mg/kg/day) has the concentration is approximately 3-fold higher in plasma than the tumor. TVB-3166 (Oral gavage; 30-100 mg/kg/day) inhibits xenograft tumor growth. The 100 and 30 mg/kg groups had plasma and tumor concentrations of 7 and 2.9 μM, respectively .

Key Properties

• CAS Number: 1533438-83-3
• MW: 384.483
• Purity: >98% (HPLC)
• Formula: C₂₄H₂₄N₄O
• SMILES: Cc1n[nH]c(c1C)-c1cc(C(=O)N2CC(C2)c2ccc(cc2)C#N)c(C)cc1C
• Target: Apoptosis
• Solubility: In Vitro: DMSO : 62.5 mg/mL (162.56 mM)

Bioactivity

• In Vivo:
  Animal model: Female BALB-c-nude mice. Dosage: 30, 60, or 100 mg/kg. Administration: Oral gavage; once daily. Result: Inhibited xenograft tumor growth. Animal model: Female BALB-c-nude mice. Dosage: 30, 60, or 100 mg/kg (Pharmacokinetic Study). Administration: Oral gavage; once daily. Result: The concentration was approximately 3-fold higher in plasma than tumor. The 100 and 30 mg/kg groups had plasma and tumor concentrations of 7 and 2.9 μM, respectively.
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• In Vitro:
  Cell Proliferation Assay Cell line: CALU-6 tumor cells. Concentration: 0.001, 0.01, 0.1, 1, 10 μM Incubation time: 24 hours. Result: Caused cell death in CALU-6 non-small-cell lung tumor cells with a cellular IC50 value of 0.10 μM. Cell Viability Assay Cell line: 90 different tumor cell lines (such as CALU-6 NSCLC cell line, NCI-H1975 NSCLC cell line). Concentration: 0.02 or 0.20 μM Incubation time: 7 days. Result: Dose-dependent induction of cell death was observed in all tumor cell lines. Western blot analysis. Cell line: COLO-205 and A549 cells. Concentration: 0.2 μM Incubation time: 48 hours. Result: Inhibited β-catenin pathway signal transduction and transcriptional activity.
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Storage & Handling

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

Quick Database Links

Gene Symbol

Apoptosis