Trifluridine/tipiracil hydrochloride mixture (Synonyms:TAS-102)
目录号 : KM11597 CAS No. : 733030-01-8 纯度 : ≥98%

Trifluridine-tipiracil hydrochloride mixture (TAS-102) 是一种新型的口服组合药物。由基于胸苷的抗肿瘤核苷类似物,三氟胸苷和有效的胸苷磷酸化酶 (thymidine phosphorylase) 抑制剂派替西西以1比0.5比例组成。

规格 价格 是否有货 数量
5mg
In-stock
10mg
In-stock
50mg
In-stock
100mg
In-stock
200mg 询价 In-stock
500mg 询价 In-stock

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生物活性

Trifluridine-tipiracil hydrochloride mixture (TAS-102) is a novel oral combination drug that consists of an antineoplastic thymidine-based nucleoside analog, trifluorothymidine, and a potent thymidine phosphorylase inhibitor, tipiracil, in a 1:0.5 molar ratio.

体外研究

Trifluridine-tipiracil hydrochloride mixture (TAS-102), a novel antimetabolite combination chemotherapy agent, consists of a rediscovered antimetabolite agent, trifluorothymidine (trifluridine, FTD) combined with the metabolic inhibitor of thymidine phosphorylase, tipiracil (TPI), in a 1:0.5 molar ratio. FTD is the active antitumor component of Trifluridine-tipiracil hydrochloride mixture (TAS-102); its monophosphate form inhibits thymidylate synthase, and its triphosphate form is incorporated into DNA in tumor cells. The incorporation into DNA is known to have antitumor effects, since the inhibition of thymidylate synthase caused by oral FTD rapidly disappears after the drug's elimination. When FTD is administered orally, it is rapidly degraded to its inactive form by thymidine phosphorylase in the intestines and liver (first-pass effect). Consequently, TPI is synthesized to maintain adequate plasma concentrations of orally-administered FTD and to potentiate the antitumor activity of FTD.

体内研究

Trifluridine-tipiracil hydrochloride mixture (TAS-102) and CPT-11 is a promising treatment option for colorectal or gastric cancer. Trifluridine-tipiracil hydrochloride mixture monotherapy has a significant antitumor activity against KM12C/5-FUFU-bearing nude mice. The combination-treated (CPT-11-and Trifluridine-tipiracil hydrochloride mixture) group is significantly superior to monotherapy. FTD systemic exposure in plasma increaseS dose-dependently. The tumor growth rate and body weight gain decreaseS dose-dependently, but FTD concentrations in the DNA of tumor tissues and white blood cells increases dose-dependently. FTD inhibits colony formation of bone marrow cells in a concentration-dependent manner.

分子式
C19H23Cl2F3N6O7
分子量
435.76
CAS号
733030-01-8
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: 

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。-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。

临床试验
科研文献
The molarity calculator equation
Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)
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