1. Metabolic Enzyme/Protease
    Apoptosis
  2. Fatty Acid Synthase (FAS)
    Apoptosis
  3. TVB-3166

TVB-3166 

Cat. No.: HY-120394 Purity: 99.55%
Handling Instructions

TVB-3166 is an orally-available, reversible, and selective fatty acid synthase (FASN) inhibitor with IC50s of 42 nM and 81 nM for FASN and cellular palmitate synthesis, respectively. TVB-3166 induces apoptosis, and inhibits in-vivo xenograft tumor growth.

For research use only. We do not sell to patients.

TVB-3166 Chemical Structure

TVB-3166 Chemical Structure

CAS No. : 1533438-83-3

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Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 110 In-stock
Estimated Time of Arrival: December 31
5 mg USD 100 In-stock
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10 mg USD 170 In-stock
Estimated Time of Arrival: December 31
50 mg USD 590 In-stock
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100 mg USD 990 In-stock
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Based on 1 publication(s) in Google Scholar

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Description

TVB-3166 is an orally-available, reversible, and selective fatty acid synthase (FASN) inhibitor with IC50s of 42 nM and 81 nM for FASN and cellular palmitate synthesis, respectively. TVB-3166 induces apoptosis, and inhibits in-vivo xenograft tumor growth[1].

IC50 & Target

IC50: 42 nM (FASN) and 81 nM (cellular palmitate synthesis)[1]

In Vitro

TVB-3166 (0.001-10 μM; 24 hours) causes cell death in CALU-6 non-small-cell lung tumor cells with a cellular IC50 value of 0.10 μM[1].
TVB-3166 (0.02 or 0.20 μM; 7 days) inhibits palmitate synthesis and tumor cell viability in a dose-dependent manner[1].
TVB-3166 (0.2 μM; 48 hours) inhibits β-catenin pathway signal transduction and transcriptional activity[1].

Cell Proliferation Assay[1]

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[1]

Cell Line: 90 different tumor cell lines
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[1]

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.
In Vivo

TVB-3166 (Oral gavage; 30-100 mg/kg/day) inhibits xenograft tumor growth[1].
TVB-3166 (Oral gavage; 30-100 mg/kg/day) has the concentration is 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[1].

Animal Model: Female BALB-c-nude mice[1]
Dosage: 30, 60, or 100 mg/kg
Administration: Oral gavage; once daily
Result: Inhibited xenograft tumor growth.
Animal Model: Female BALB-c-nude mice[1]
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.
Molecular Weight

384.47

Formula

C₂₄H₂₄N₄O

CAS No.

1533438-83-3

SMILES

N#CC1=CC=C(C2CN(C(C3=CC(C4=NNC(C)=C4C)=C(C)C=C3C)=O)C2)C=C1.

Shipping

Room temperature in continental US; may vary elsewhere

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 62.5 mg/mL (162.56 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.6010 mL 13.0049 mL 26.0098 mL
5 mM 0.5202 mL 2.6010 mL 5.2020 mL
10 mM 0.2601 mL 1.3005 mL 2.6010 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (5.41 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: 2.08 mg/mL (5.41 mM); Suspended solution; Need ultrasonic

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (5.41 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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TVB-3166
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