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

TVB-3166 

目录号: HY-120394 纯度: 99.55%
产品使用指南

TVB-3166 是一种口服有效,可逆和选择性脂肪酸合成酶 (FASN) 抑制剂,对于 FASN 和细胞棕榈酸酯合成的 IC50 分别为 42 nM 和 81 nM。TVB-3166 诱导细胞凋亡,并抑制体内异种移植肿瘤的生长。

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TVB-3166 Chemical Structure

TVB-3166 Chemical Structure

CAS No. : 1533438-83-3

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Size Price Stock Quantity
Free Sample (0.1-0.5 mg)   Apply now  
10 mM * 1 mL in DMSO ¥1100 In-stock
5 mg ¥1000 In-stock
10 mg ¥1700 In-stock
50 mg ¥5900 In-stock
100 mg ¥9900 In-stock
200 mg   Get quote  
500 mg   Get quote  

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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
* 请根据产品在不同溶剂中的溶解度,选择合适的溶剂配制储备液,并请注意储备液的保存方式和期限。
In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案,配制前请先配制澄清的储备液,再依次添加助溶剂 (为保证实验结果的可靠性,体内实验的工作
液,建议您现用现配,当天使用;澄清的储备液可以根据储存条件,适当保存;以下溶剂前的百分比是指该溶剂在您配制终溶液中的体积占比):

  • 1.

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

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

  • 2.

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

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

  • 3.

    请依序添加每种溶剂: 10% DMSO    90% corn oil

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

*以上所有助溶剂都可在 MCE 网站选购。
References
  • 摩尔计算器

  • 稀释计算器

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This equation is commonly abbreviated as: C1V1 = C2V2

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× = ×
C1   V1   C2   V2

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产品名称:
TVB-3166
目录号:
HY-120394
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