Tipiracil hydrochloride(Synonyms: 盐酸替吡嘧啶) 目录号 : GC14473
A potent TPase inhibitor
Sample solution is provided at 25 µL, 10mM.
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|Animal experiment :|
Xenograft-bearing nude mouse models of colorectal and gastric cancers
150 mg/kg/day (combination of Trifluridine and Tipiracil Hydrochloride); p.o.; b.i.d., for 14 days
The tumor growth-inhibitory activity and RTV5 in mice administered TAS-102 (consisting of Trifluridine and Tipiracil Hydrochloride) with Oxaliplatin were significantly superior to those associated with either monotherapy in mice with colorectal (HCT 116 and SW-48 cells) and gastric (SC-2 and MKN74 cells) cancers. In vivo, TAS-102 alone was effective in MKN74/5FU cells, and its anti-tumor activity was substantially enhanced in combination with Oxaliplatin. No significant decrease in body weight or toxicity was observed compared to either monotherapy.
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.
. Tsukihara H, Nakagawa F, Sakamoto K et al. Efficacy of combination chemotherapy using a novel oral chemotherapeutic agent, TAS-102, together with bevacizumab, cetuximab, or panitumumab on human colorectal cancer xenografts. Oncol Rep. 2015 May;33(5):2135-42.
Tipiracil is an inhibitor of Thymidine phosphorylase (TP).
Thymidine phosphorylase (TP)is a key enzyme in the pyrimidine nucleoside salvage pathway. It catalyses the reversible phosphorylation of thymidine, and thereby generate thymine and 2-deoxy-D-ribose-1-phosphate.
Tipiracil (TPI) and trifluridine (FTD) are active components of TAS-102 at a molecular ratio of 1:0.5, which is a novel oral nucleoside antitumor agent in clinical trials. Oral administered TPI and FTD co-treatment may differ from that of i.v. administration of FTD alone.  When FTD is administered orally, it is rapidly degraded to its inactive form in the intestines and the liver (first-pass effect) , but the combination with TPI helps to maintain adequate FTD plasma concentrations . TPI thus, potentiates the antitumor activity of FTD, and the optimal molecular ratio of FTD to TPI has been proven to be 1:0.5. 
1. Tsukihara H1, Nakagawa F2, Sakamoto K et al. Efficacy of combination chemotherapy using a novel oral chemotherapeutic agent, TAS-102, together with bevacizumab, cetuximab, or panitumumab on human colorectal cancer xenografts. Oncol Rep. 2015 May;33(5):2135-42.
2. Dexter DL, Wolberg WH, Ansfield FJ, Helson L and Heidelberger C: The clinical pharmacology of 5-trifluoro-methyl-2'-deoxyuridine. Cancer Res 32: 247-253, 1972.
3. Fukushima M, Suzuki N, Emura T et al. Structure and activity of specific inhibitors of thymidine phosphorylase to potentiate the function of antitumor 2'-deoxyribonucleosides. biochem Pharmacol 59: 1227-1236, 2000.
|溶解度||≥ 13.25 mg/mL in Water||储存条件||Store at -20°C|
|General tips||For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.|
|Shipping Condition||Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
|% DMSO % % Tween 80 % ddH2O|
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL ddH2O，混匀澄清。
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