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Trifluridine/tipiracil hydrochloride mixture

产品编号 T3658 CAS 733030-01-8

别名: Trifluridine-tipiracil hydrochloride mixture, TAS102, TAS-102, TAS 102

Trifluridine/tipiracil hydrochloride mixture (TAS-102) 是一种新型口服组合药物，含有摩尔比为 2:1 的曲氟尿苷(TFT) 和盐酸替吡嘧啶 (TTP)。它主要通过抑制胸苷酸合酶 (TS) 和掺入 DNA 来显示抗肿瘤活性。

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Trifluridine/tipiracil hydrochloride mixture Chemical Structure

Trifluridine/tipiracil hydrochloride mixture, CAS 733030-01-8

规格	价格/CNY	货期
1 mg	￥ 232	现货
2 mg	￥ 297	现货
5 mg	￥ 413	现货
10 mg	￥ 663	现货
25 mg	￥ 1,190	现货
50 mg	￥ 1,980	现货
100 mg	￥ 3,160	现货
200 mg	￥ 4,530	现货
500 mg	￥ 6,870	现货
1 mL * 10 mM (in DMSO)	￥ 668	现货

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生物活性

化学信息

存储 & 溶解度

参考文献

相关产品

产品描述	Trifluridine/tipiracil hydrochloride mixture (TAS-102) is a novel oral combination drug containing trifluridine (TFT) and Tipiracil hydrochloride (TTP) in a molar ratio of 2:1.
体外活性	TAS-102 is an oral combination drug consisting of trifluridine (FTD), which is a thymidine-based nucleoside analog, and tipiracil hydrochloride (TPI), which improves the bioavailability of FTD by inhibiting its catabolism by thymidine phosphorylase (TP)[1]. Phosphorylated form of trifluridine is incorporated into DNA resulting in DNA dysfunction and cell cycle arrest. Thymidine phosphorylase inhibitor inhibits degradation of FTD and inhibits angiogenesis. Thus, TAS-102 treatment results in massive trifluridine incorporation into DNA and in activation of similar DNA damage response pathways, which involve phosphorylation of Chk1 and cycle arrest during the G2/M-phase[2].
体内活性	The elimination half-life of FTD after intravenous administration to humans is very rapid (18 minutes), due to the rapid degradation of FTD to its major metabolite, 5-trifluoromethyl-2,4(1H,3H)-pyrimidinedione. In monkeys, the plasma FTD level after oral administration alone is very low, suggesting extensive first-pass metabolism by the liver and intestine TPase. However, the addition of TPI(tipiracil hydrochloride) is found to enable oral administration. By inhibiting TP, TPI inhibits the degradation of FTD in the liver and intestines following oral administration and thereby improves its bioavailability. The TP enzyme catalyzes the phosphorolysis of pyrimidine 2'-deoxynucleosides such as FTD. Studies using human CRC tumor xenografts in mice determine that the maximum antitumor activity is achieved with a 1:0.5 molar ratio, and studies in mice and monkeys show that the maximum plasma concentration of FTD is almost achieved with the same ratio. Moreover, this ratio produces a favorable balance between antitumor activity and toxicity. Lower toxicity in mice is observed with TPI coadministration than with FTD alone. TAS-102 (FTD) can overcome acquired resistance to 5-FU because the main mechanism of TAS-102 is not associated with main metabolic enzymes of 5-FU, such as TS and OPRT. TAS-102 has demonstrated efficacy in 5-FU-refractory cancers[1].
激酶实验	IC50 determination of compounds against EGFR enzymes: The inhibition potency of compounds against EGFR WT and mutant enzymes is assessed using CisBio homogenous time resolved fluorescence approach (HTRF, Cat No. 62TK0PEJ) according to manufacturer's instruction. The final enzyme concentrations used in this assay are 0.1 nM, 0.03 nM, and 0.026 nM for EGFR wild type, L858R and Exon19Del, respectively, and 0.8 μM, 4 μM and 25 μM ATP, corresponding to the Km values of EGFR enzymes, are applied accordingly. In brief, 3 μL of ATP and 2 μM TK biotin-peptide substrate are incubated in the presence or absence of serially diluted compound at room temperature in 384-well Greiner white polystyrene assay plates. The reaction is initiated by addition of 3 μL kinase which could phosphorylate the substrate peptide, and the assay buffer contains 1 mM DTT, 5 mM MgCl2, 1 mM MnCl2, and 0.01% CHAPS. After 30 minutes incubation, the reaction is stopped by the addition of 6 μl detection reagent mix containing 250 nM Strep-XL665 and TK Ab Europium Cryptate diluted in detection buffer. The plates are incubated for 1 h before the fluorescence is then measured at 615 nm and 665 nm, respectively with excitation wavelength at 320 nm by EnVision Multilabel Reader from Perkin Elmer using standard HTRF settings. The calculated signal ratio of 665 nm/615 nm is proportional to the kinase activity. The concentration of compound producing 50% inhibition of the respective kinase (IC50) is calculated using four-parameter logistic fit.

别名	Trifluridine-tipiracil hydrochloride mixture, TAS102, TAS-102, TAS 102
分子量	871.53
分子式	C29H34Cl2F6N8O12
CAS No.	733030-01-8

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

Ethanol: 100 mg/mL (114.74 mM)

DMSO: 100 mg/mL (114.74 mM), Sonication is recommended.

溶液配制表

可选溶剂	浓度体积质量	1 mg	5 mg	10 mg	25 mg
Ethanol / DMSO	1 mM	1.1474 mL	5.737 mL	11.4741 mL	28.6852 mL
	5 mM	0.2295 mL	1.1474 mL	2.2948 mL	5.737 mL
	10 mM	0.1147 mL	0.5737 mL	1.1474 mL	2.8685 mL
	20 mM	0.0574 mL	0.2869 mL	0.5737 mL	1.4343 mL
	50 mM	0.0229 mL	0.1147 mL	0.2295 mL	0.5737 mL
	100 mM	0.0115 mL	0.0574 mL	0.1147 mL	0.2869 mL

计算器

摩尔浓度计算器

稀释计算器

配液计算器

分子量计算器

质量

浓度

容积

分子量

浓度 (起始)

容积 (起始)

浓度 (终)

容积 (终)

溶液体积

质量

配液浓度

参考文献

1. Lenz HJ, et al. Cancer Treat Rev. 2015, 41(9):777-83. 2. Nukatsuka M, et al. Anticancer Res. 2015, 35(9):4605-15.

文献引用

1. Luo P Q, Zhang L X, Chen Z M, et al.Effects and mechanisms of trifluridine alone or in combination with cryptotanshinone in inhibiting malignant biological behavior of gastric cancer.Cell Cycle.2023: 1-15.

剂量换算

对于不同动物的给药剂量换算，您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

第一步：请输入动物实验的基本信息

剂量

mg/kg

每只动物体重

给药体积

μL

动物数量

第二步：请输入动物体内配方组成，不同的产品配方组成不同，如有配方需求，可先联系我们提供正确的体内配方。

% DMSO+

% +

% Tween 80+

% ddH₂O

%DMSO+

计算重置

计算结果如下:

工作液浓度: mg/ml;

母液配置方法: mg 药物溶于 μL DMSO (母液浓度为 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 μL DMSO 主液，加入 μL PEG300，混匀澄清，再加 μL Tween 80，混匀澄清，再加 μL ddH₂O, 混匀澄清。

备注:

要按顺序从左向右依次添加助溶剂。可配合物理方法，如涡流、超声波或热水浴使之帮助溶解。

技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到，包括如何准备库存溶液，如何存储产品，以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

Trifluridine/tipiracil hydrochloride mixture 733030-01-8 Cell Cycle/Checkpoint DNA Damage/DNA Repair Nucleoside Antimetabolite/Analog DNA/RNA Synthesis inhibit Trifluridine-tipiracil hydrochloride mixture Thymidylate Synthase oral Inhibitor FTD DNA nucleoside TAS102 TAS-102 antitumor TAS 102 TPI inhibitor

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Trifluridine/tipiracil hydrochloride mixture

存储

溶解度

溶液配制表

计算器

输入分子式，点击计算，可计算出产品的分子量。

参考文献

文献引用

相关产品

相关化合物库

剂量换算

体内实验配液计算器

技术支持

Keywords