TAS-102

    
≥98%

TAS-102

源叶(MedMol)
S81525 一键复制产品信息
733030-01-8
C19H23Cl2F3N6O7
575.32
货号 规格 价格 上海 北京 武汉 南京 购买数量
S81525-5mg ≥98% ¥486.00 5 - - -
S81525-25mg ≥98% ¥625.00 7 - - -
S81525-100mg ≥98% ¥900.00 8 - - -
产品介绍 参考文献 质检证书(COA) 摩尔浓度计算器 相关产品

产品介绍

TAS-102 is a novel oral combination drug containing trifluridine (TFT) and Tipiracil hydrochloride (TTP) in a molar ratio of 2:1.

产品描述:

TAS-102 is a novel oral combination drug containing trifluridine (TFT) and Tipiracil hydrochloride (TTP) in a molar ratio of 2:1.

靶点: DNA/RNA Synthesis;Nucleoside Antimetabolite/Analog;NucleosideAntimetabolite/Analog; DNA/RNASynthesis
体外研究: 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
体内研究: 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
参考文献: 1. Nukatsuka M, et al. Efficacy of Combination Chemotherapy Using a Novel Oral Chemotherapeutic Agent, TAS-102, with Oxaliplatin on Human Colorectal and Gastric Cancer Xenografts. Anticancer Res. 2015, 35(9):4605-15. 2. Lenz HJ, et al. TAS-102, a novel antitumor agent: a review of the mechanism of action. Cancer Treat Rev. 2015, 41(9):777-83.
溶解性: Soluble  in  DMSO、Ethanol
保存条件: -20°C;充氩
配置溶液浓度参考:
1mg 5mg 10mg
1 mM 1.738 ml 8.691 ml 17.382 ml
5 mM 0.348 ml 1.738 ml 3.476 ml
10 mM 0.174 ml 0.869 ml 1.738 ml
50 mM 0.035 ml 0.174 ml 0.348 ml
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参考文献

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