TAS-114|cas:1198221-21-4|西域试剂

TAS-114,99.54%

产品编号：Bellancom-124062| CAS NO：1198221-21-4| 分子式：C₂₁H₂₉N₃O₆S| 分子量：451.54

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货号	价格	库存与货期
Bellancom-124062	￥990.00	杭州北京（现货）
Bellancom-124062	￥2900.00	杭州北京（现货）
Bellancom-124062	￥4600.00	杭州北京（现货）
Bellancom-124062	￥14000.00	杭州北京（现货）

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TAS-114

产品介绍

TAS-114 是一种具有口服活性的 dUTPase 和 二氢嘧啶脱氢酶 (DPD) 的双靶点抑制剂，可提高氟嘧啶活性分子的疗效。

生物活性

TAS-114 is an orally active dual dUTPase/dihydropyrimidine dehydrogenase (DPD) inhibitor, can improving the therapeutic efficacy of fluoropyrimidine.

体外研究

TAS-114 (1-10 μM; 72 hours) increases the cytotoxicity of 5-Fluorouracil (5-FU) and 5-FU,2′-deoxy-5-fluorouridine (FdUrd) against various cancer cell lines in dose-dependent manner.

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

Cell Cytotoxicity Assay

Cell Line:	HeLa, NUGC-4, NCI-H441, HT-29, CFPAC-1, and MCF-7 cell lines
Concentration:	72 hours
Incubation Time:	1 μM, 3 μM, and 10 μM
Result:	Clearly increased the cytotoxicity of FdUrd and 5-FU against various cancer cell lines in dose-dependent manner.

体内研究
(In Vivo)

TAS-114 (37.5-1,200 mg/kg/day; orally; 1-14 days) increases the antitumor activity of 5-FU when co-administers with Capecitabine (539 mg/kg/day) in mice.

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

Animal Model:	BALB/c nude mice with MX-1 human breast cancer xenografts
Dosage:	37.5 to 1,200 mg/kg/day
Administration:	Orally; daily; 1-14 days
Result:	Decreased the tolerable doses of Capecitabine (539 mg/kg/day) in a dose-dependent manner in mice.

体内研究

TAS-114 (37.5-1,200 mg/kg/day; orally; 1-14 days) increases the antitumor activity of 5-FU when co-administers with Capecitabine (539 mg/kg/day) in mice.

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

Animal Model:	BALB/c nude mice with MX-1 human breast cancer xenografts
Dosage:	37.5 to 1,200 mg/kg/day
Administration:	Orally; daily; 1-14 days
Result:	Decreased the tolerable doses of Capecitabine (539 mg/kg/day) in a dose-dependent manner in mice.

体内研究

TAS-114 (37.5-1,200 mg/kg/day; orally; 1-14 days) increases the antitumor activity of 5-FU when co-administers with Capecitabine (539 mg/kg/day) in mice.

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

Animal Model:	BALB/c nude mice with MX-1 human breast cancer xenografts
Dosage:	37.5 to 1,200 mg/kg/day
Administration:	Orally; daily; 1-14 days
Result:	Decreased the tolerable doses of Capecitabine (539 mg/kg/day) in a dose-dependent manner in mice.

性状

Solid

溶解性数据

In Vitro:

DMSO : 100 mg/mL (221.46 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.2146 mL	11.0732 mL	22.1464 mL
5 mM	0.4429 mL	2.2146 mL	4.4293 mL
10 mM	0.2215 mL	1.1073 mL	2.2146 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 (stored under nitrogen)。-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: ≥ 2.5 mg/mL (5.54 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (5.54 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 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: ≥ 2.5 mg/mL (5.54 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (5.54 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
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.5 mg/mL (5.54 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (5.54 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 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。