标签归档：trifluridine

生物活性分子抑制剂Trifluridine(Synonyms: 曲氟尿苷; Trifluorothymidine; 5-Trifluorothymidine; TFT)

发表于由

生物活性分子抑制剂 特异性抑制剂 激动剂 化合物库 重组蛋白 Trifluridine (Synonyms: 曲氟尿苷; Trifluorothymidine; 5-Trifluorothymidine; TFT) 纯度: 99.72%

Trifluridine (Trifluorothymidine; 5-Trifluorothymidine; TFT) 是不可逆的胸苷酸合酶抑制剂，从而抑制 DNA合成。Trifluridine 是用于单纯疱疹病毒 (HSV) 感染的抗病毒药物。

Trifluridine(Synonyms: 曲氟尿苷; Trifluorothymidine; 5-Trifluorothymidine; TFT)

Trifluridine Chemical Structure

CAS No. : 70-00-8

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 ￥716 In-stock
50 mg ￥651 In-stock
100 mg ￥976 In-stock
200 mg ￥1488 In-stock
500 mg   询价  
1 g   询价  

* Please select Quantity before adding items.

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生物活性

Trifluridine (Trifluorothymidine; 5-Trifluorothymidine; TFT) is an irreversible thymidylate synthase inhibitor, and thereby suppresses DNA synthesis. Trifluridine is an antiviral drug for herpes simplex virus (HSV) infection.

IC50 & Target

HSV-1

 

HSV-2

 

Thymidylate Synthase

 

Nucleoside Antimetabolite/Analog

 

Clinical Trial

分子量

296.20

Formula

C10H11F3N2O5
CAS 号

70-00-8
中文名称

三氟尿苷；三氟甲苷；三氟胸苷；三氟甲尿苷；三氟哩啶；三氟胸腺嘧啶核苷；曲氟尿苷；屈氟尿苷
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 : ≥ 100 mg/mL (337.61 mM)

* “≥” means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.3761 mL 16.8805 mL 33.7610 mL
5 mM 0.6752 mL 3.3761 mL 6.7522 mL
10 mM 0.3376 mL 1.6880 mL 3.3761 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: ≥ 2.5 mg/mL (8.44 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (8.44 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 (8.44 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (8.44 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 (8.44 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (8.44 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 25.0 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]. Suzuki N, et al. Mode of action of trifluorothymidine (TFT) against DNA replication and repair enzymes. Int J Oncol. 2011 Jul;39(1):263-70.

    [2]. Suzuki N, et al. Trifluorothymidine exhibits potent antitumor activity via the induction of DNA double-strand breaks. Exp Ther Med. 2011 May;2(3):393-397.

    [3]. Temmink OH, et al. Irinotecan-induced cytotoxicity to colon cancer cells in vitro is stimulated by pre-incubation withtrifluorothymidine. Eur J Cancer. 2007 Jan;43(1):175-83.

    [4]. Okayama T, et al. Involvement of concentrative nucleoside transporter 1 in intestinal absorption of trifluorothymidine, a novel antitumor nucleoside, in rats. J Pharmacol Exp Ther. 2012 Feb;340(2):457-62.

    [5]. Novel trifluridine crystal form and preparation method thereof. CN105198946A.

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Trifluridine/tipiracil hydrochloride mixture(Synonyms: TAS-102)

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

Trifluridine/tipiracil hydrochloride mixture (Synonyms: TAS-102) 纯度: ≥98.0%

Trifluridine/tipiracil hydrochloride mixture (TAS-102) 是一种有效且具有口服活性的核苷类抗肿瘤剂。Trifluridine/tipiracil hydrochloride mixture (TAS-102) 的组成是 1:0.5 的混合物 (以摩尔计) α,α,α-三氟胸苷 (FTD) 和胸苷磷酸化酶抑制剂 (TPI)。Trifluridine/tipiracil hydrochloride mixture (TAS-102) 主要通过抑制胸苷酸合酶 (TS) 和掺入 DNA 来显示抗肿瘤活性。

Trifluridine/tipiracil hydrochloride mixture(Synonyms: TAS-102)

Trifluridine/tipiracil hydrochloride mixture Chemical Structure

CAS No. : 733030-01-8

规格 价格 是否有货 数量
10 mM * 1 mL in Water ￥770 In-stock
5 mg ￥700 In-stock
10 mg ￥1100 In-stock
50 mg ￥3400 In-stock
100 mg ￥4700 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

Trifluridine/tipiracil hydrochloride mixture 相关产品

•相关化合物库:

  • Covalent Screening Library Plus
  • Drug Repurposing Compound Library Plus
  • FDA-Approved Drug Library Plus
  • FDA-Approved Drug Library Mini
  • Bioactive Compound Library Plus
  • Apoptosis Compound Library
  • Cell Cycle/DNA Damage Compound Library
  • FDA-Approved Drug Library
  • Anti-Cancer Compound Library
  • Anti-Aging Compound Library
  • Drug Repurposing Compound Library
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  • Anti-COVID-19 Compound Library
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  • Anti-Lung Cancer Compound Library
  • Anti-Blood Cancer Compound Library
  • Anti-Cancer Metabolism Compound Library

生物活性

Trifluridine/tipiracil hydrochloride mixture (TAS-102) is a potent and orally active nucleoside antitumor agent. The composition of Trifluridine/tipiracil hydrochloride mixture (TAS-102) is a 1:0.5 mixture (on a molar basis) of alpha,alpha,alpha-tri-fluorothymidine (FTD) and thymidine phosphorylase inhibitor (TPI). Trifluridine/tipiracil hydrochloride mixture (TAS-102) shows the antitumor activity mainly via the inhibition of thymidylate synthase (TS) and incorporation into DNA[1][2].

体内研究
(In Vivo)

Trifluridine/tipiracil hydrochloride mixture (150 mg/kg/day; p.o.; twice a day for 14 days) prevents body weight loss and reduces the relative tumor volume in colorectal cancer and gastric cancer mice models[2].

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: Male nude mice bearing KM12C, KM12C/5-FU, DLD-1, DLD-1/5-FU, and SC-2 cells[2]
Dosage: 150 mg/kg/day
Administration: p.o.; twice a day for 14 days
Result: Prevented body weight loss and reduced the relative tumor volume in colorectal cancer and gastric cancer mice models.

Clinical Trial

分子量

435.76

Formula

C29H34Cl2F6N8O12
CAS 号

733030-01-8
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
溶解性数据
In Vitro: 

H2O : 100 mg/mL (229.48 mM; Need ultrasonic)

DMF : 20 mg/mL (45.90 mM; Need ultrasonic)

DMSO : 2.34 mg/mL (5.37 mM; Need ultrasonic and warming)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.2948 mL 11.4742 mL 22.9484 mL
5 mM 0.4590 mL 2.2948 mL 4.5897 mL
10 mM 0.2295 mL 1.1474 mL 2.2948 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 (sealed storage, away from moisture)。-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。
参考文献

  • [1]. Emura T, et al. A novel antimetabolite, TAS-102 retains its effect on FU-related resistant cancer cells. Int J Mol Med. 2004;13(4):545-549.

    [2]. Nukatsuka M, et al. Efficacy of combination chemotherapy using a novel oral chemotherapeutic agent, TAS-102, with irinotecan hydrochloride on human colorectal and gastric cancer xenografts. Anticancer Res. 2015;35(3):1437-1445.

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