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

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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  

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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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