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

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

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TVB-3166 Chemical Structure

TVB-3166 Chemical Structure

CAS No. : 1533438-83-3

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10 mM * 1 mL in DMSO
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Based on 6 publication(s) in Google Scholar

TVB-3166 Related Antibodies

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  • Biological Activity

  • Purity & Documentation

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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 biochemical 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

ISX-9 promotes neurogenesis in vivo, enhancing the proliferation and differentiation of hippocampal subgranular zone (SGZ) neuroblasts, and the dendritic arborization of adult-generated dentate gyrus neurons. At 2.5-20 μM, ISX-9 has been shown to dose-dependently trigger neurogenesis and block gliogenesis in adult rat hippocampal stem cells through a calcium-activated signaling pathway dependent on myocyte-enhancer factor 2-dependent gene expression[1].
Molecular exploration of ISX-9-induced regulation of neurogenesis (via FACS and microarray of SGZ stem and progenitor cells) suggested the involvement of the myocyte-enhancer family of proteins (Mef2)[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

TVB-3166 Related Antibodies

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 (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[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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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.
Appearance

Solid

Color

White to off-white

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 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 62.5 mg/mL (162.56 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
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Concentration
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Volume
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 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

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 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

    This protocol yields a suspended solution of 2.08 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.76%

COA (247 KB) LCMS (266 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.6010 mL 13.0049 mL 26.0098 mL 65.0246 mL
5 mM 0.5202 mL 2.6010 mL 5.2020 mL 13.0049 mL
10 mM 0.2601 mL 1.3005 mL 2.6010 mL 6.5025 mL
15 mM 0.1734 mL 0.8670 mL 1.7340 mL 4.3350 mL
20 mM 0.1300 mL 0.6502 mL 1.3005 mL 3.2512 mL
25 mM 0.1040 mL 0.5202 mL 1.0404 mL 2.6010 mL
30 mM 0.0867 mL 0.4335 mL 0.8670 mL 2.1675 mL
40 mM 0.0650 mL 0.3251 mL 0.6502 mL 1.6256 mL
50 mM 0.0520 mL 0.2601 mL 0.5202 mL 1.3005 mL
60 mM 0.0433 mL 0.2167 mL 0.4335 mL 1.0837 mL
80 mM 0.0325 mL 0.1626 mL 0.3251 mL 0.8128 mL
100 mM 0.0260 mL 0.1300 mL 0.2601 mL 0.6502 mL
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TVB-3166 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

TVB-31661533438-83-3TVB3166TVB 3166Fatty Acid Synthase (FASN)ApoptosisInhibitorinhibitorinhibit

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