TVB-3664|cas:2097262-58-1|西域试剂

TVB-3664,99.57%

产品编号：Bellancom-120062| CAS NO：2097262-58-1| 分子式：C₂₅H₂₃F₃N₄O₂| 分子量：468.47

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-120062	￥3780.00	杭州北京（现货）
Bellancom-120062	￥6300.00	杭州北京（现货）
Bellancom-120062	￥11250.00	杭州北京（现货）
Bellancom-120062	￥18000.00	杭州北京（现货）
Bellancom-120062	￥27000.00	杭州北京（现货）

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TVB-3664

产品介绍

TVB-3664 是具有口服活性的、可逆的、有效的、选择性的并具有高生物利用度的脂肪酸合酶 (FASN) 抑制剂，其对人和老鼠棕榈酸酯合成的 IC₅₀ 值分别为 18 nM 和 12 nM。可显著降低微管蛋白棕榈酰化和 mRNA表达。

生物活性

TVB-3664 is an orally available, reversible, potent, selective and highly bioavailable fatty acid synthase (FASN) inhibitor, with IC₅₀ values of 18 nM and 12 nM for human and mouse cell palmitate synthesis, respectively. TVB-3664 significantly reduces tubulin palmitoylation and mRNA expression.

体外研究

TVB-3664 (0-1 μM, 7 days) shows anti-tumor activity in CaCo2, HT29 and LIM2405 cell lines.
TVB-3664 decreases viability in multiple tumor cell lines from solid and hematopoietic tumor types.

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

Cell Proliferation Assay

Cell Line:	CaCo2, HT29 and LIM2405 cell lines.
Concentration:	0-1 μM.
Incubation Time:	7 days.
Result:	Showed anti-tumor activity.

体内研究
(In Vivo)

TVB-3664 (3 mg/kg (Pt 2614 and Pt 2449PT) or 6 mg/kg (Pt 2402 and Pt 2449LM), oral gavage, daily, 4 weeks) treatment leads to a significant reduction in tumor volume and tumor weight in Pt 2614, Pt 2449PT, and Pt 2402 PDX models, with an average reduction in tumor weight of 30%, 37.5% and 51.5%, respectively.

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

Animal Model:	Colorectal cancer (CRC) PDX models in NOD-SCID-IL2rg-/- (NSG) mice using specimens collected from patients who had undergone surgery for resection of primary CRC or CRC metastasis.
Dosage:	3 mg/kg (Pt 2614 and Pt 2449PT) or 6 mg/kg (Pt 2402 and Pt 2449LM).
Administration:	Oral gavage daily for 4 weeks.
Result:	Led to a significant reduction in tumor volume and tumor weight in Pt 2614, Pt 2449PT, and Pt 2402 PDX models, with an average reduction in tumor weight of 30%, 37.5% and 51.5%, respectively.

体内研究

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

Animal Model:	Colorectal cancer (CRC) PDX models in NOD-SCID-IL2rg-/- (NSG) mice using specimens collected from patients who had undergone surgery for resection of primary CRC or CRC metastasis.
Dosage:	3 mg/kg (Pt 2614 and Pt 2449PT) or 6 mg/kg (Pt 2402 and Pt 2449LM).
Administration:	Oral gavage daily for 4 weeks.
Result:	Led to a significant reduction in tumor volume and tumor weight in Pt 2614, Pt 2449PT, and Pt 2402 PDX models, with an average reduction in tumor weight of 30%, 37.5% and 51.5%, respectively.

体内研究

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

Animal Model:	Colorectal cancer (CRC) PDX models in NOD-SCID-IL2rg-/- (NSG) mice using specimens collected from patients who had undergone surgery for resection of primary CRC or CRC metastasis.
Dosage:	3 mg/kg (Pt 2614 and Pt 2449PT) or 6 mg/kg (Pt 2402 and Pt 2449LM).
Administration:	Oral gavage daily for 4 weeks.
Result:	Led to a significant reduction in tumor volume and tumor weight in Pt 2614, Pt 2449PT, and Pt 2402 PDX models, with an average reduction in tumor weight of 30%, 37.5% and 51.5%, respectively.

性状

Solid

溶解性数据

In Vitro:

DMSO : 10 mg/mL (21.35 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.1346 mL	10.6730 mL	21.3461 mL
5 mM	0.4269 mL	2.1346 mL	4.2692 mL
10 mM	0.2135 mL	1.0673 mL	2.1346 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 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.5 mg/mL (5.34 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (5.34 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 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
2.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.08 mg/mL (4.44 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (4.44 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
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.08 mg/mL (4.44 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (4.44 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。