TAS-102 TAS-102 (Trifluridine-Tipiracil Hydrochloride Mixture) is an orally administered combination of a thymidine-based nucleic acid analogue, trifluridine , and a thymidine phosphorylase inhibitor, tipiracil hydrochloride .

In vitro

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). 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.

In vivo

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.

规格

英文别名

Tipiracil-trifluridine Mixture (2:1) | trifluridine (TFT) and Tipiracil Hydrochloride (TTP) in molar ratio of 1: 0.5 | Trifluridine-tipiracil Hydrochloride Mixture | Trifluridine-Tipiracil Hydrochloride MixtureThymidine,α,α,α-trifluoro-,mixt. with 5-

规格或纯度

10mM in DMSO

英文名称

TAS-102

生化机理

TAS-102（三氟尿苷-盐酸替吡嘧啶混合物）是胸腺嘧啶核酸类似物三氟尿苷和胸腺嘧啶磷酸化酶抑制剂盐酸替吡嘧啶的口服复方制剂。

储存条件

-80℃储存

运输条件

特低温运输

名称和识别符

分子类型

小分子

分子量

871.52

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化学和物理性质

敏感性

易吸潮

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GHS07

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H302: 吞食有害

H315: 引起皮肤刺激

H319: 引起严重眼睛刺激

H335: 可能引起呼吸道刺激

预防措施声明

P261: 避免吸入灰尘/烟雾/气体/雾/蒸汽/喷雾

P305+P351+P338: 如进入眼睛：用水小心冲洗几分钟。如戴隐形眼镜并可方便地取出，取出隐形眼镜。继续冲洗。

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常见问题

本产品应如何储存？

请于?80 °C条件下保存。需超低温保存以维持规定的有效期。

本产品如何运输？

本产品采用干冰配冷袋冷冻运输。收货后请立即拆包，并按上述储存条件保存；处理干冰时请戴隔热手套并保持通风。

本产品的 CAS 号、分子式和分子量是多少？

本产品的 CAS 号为 733030-01-8，分子式为 [C9H11ClN4O2? (HCl)] ? 2[ C10H11F3N2O5]，分子量为 871.52 g/mol。

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