TVB-3166|cas:1533438-83-3|西域试剂

TVB-3166,99.76%

产品编号：Bellancom-120394| CAS NO：1533438-83-3| 分子式：C₂₄H₂₄N₄O| 分子量：384.47

本网站销售的所有产品仅用于工业应用或者科学研究等非医疗目的,不可用于人类或动物的临床诊断或者治疗,非药用,非食用，

货号	价格	库存与货期
Bellancom-120394	￥1000.00	杭州北京（现货）
Bellancom-120394	￥1700.00	杭州北京（现货）
Bellancom-120394	￥5200.00	杭州北京（现货）
Bellancom-120394	￥9000.00	杭州北京（现货）

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TVB-3166

产品介绍

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。

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.

体外研究

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.
TVB-3166 (0.02 or 0.20 μM; 7 days) inhibits palmitate synthesis and tumor cell viability in a dose-dependent manner.
TVB-3166 (0.2 μM; 48 hours) inhibits β-catenin pathway signal transduction and transcriptional activity.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

体内研究
(In Vivo)

TVB-3166 (Oral gavage; 30-100 mg/kg/day) inhibits xenograft tumor growth.
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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

性状

Solid

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。