TVB-3166

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TVB-3166  纯度: 99.76%

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。

TVB-3166

TVB-3166 Chemical Structure

CAS No. : 1533438-83-3

规格 价格 是否有货 数量
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
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500 mg   询价  

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TVB-3166 相关产品

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生物活性

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]
体外研究
(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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

体内研究
(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].

上海金畔生物科技有限公司 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.

分子量

384.47

Formula

C24H24N4O
CAS 号

1533438-83-3
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

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

配制储备液
浓度 溶剂体积 质量 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；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

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。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

  • 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

    此方案可获得 ≥ 2.08 mg/mL (5.41 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

  • 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

    此方案可获得 2.08 mg/mL (5.41 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。

    以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
  • 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

    此方案可获得 ≥ 2.08 mg/mL (5.41 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献

  • [1]. Ventura R, et al. Inhibition of de novo Palmitate Synthesis by Fatty Acid Synthase Induces Apoptosis in Tumor Cells by Remodeling Cell Membranes, Inhibiting Signaling Pathways, and Reprogramming Gene Expression. EBioMedicine. 2015 Jul 2;2(8):808-24.

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