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Tipiracil hydrochloride

现货
Catalog No.
A3875
胸苷磷酸化酶抑制剂
组合的产品项目
规格价格库存 数量
10mM (in 1mL H2O)
¥ 1,050.00
现货
5mg
¥ 1,000.00
现货
10mg
¥ 1,420.00
现货
25mg
¥ 2,710.00
现货
50mg
¥ 3,710.00
现货

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Background

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. [1] When FTD is administered orally, it is rapidly degraded to its inactive form in the intestines and the liver (first-pass effect) [2], but the combination with TPI helps to maintain adequate FTD plasma concentrations [3]. 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. [3]

References:
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.

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt279.12
Cas No.183204-72-0
FormulaC9H12Cl2N4O2
SynonymsTipiracil
Solubility<2.26 mg/mL in DMSO, <2.64 mg/mL in EtOH, ≥13.25 mg/mL in H2O
Chemical Name5-chloro-6-[(2-iminopyrrolidin-1-yl)methyl]-1H-pyrimidine-2,4-dione;hydrochloride
SDFDownload SDF
Canonical SMILESC1CC(=N)N(C1)CC2=C(C(=O)NC(=O)N2)Cl.Cl
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

试验操作

动物实验 [1]:

动物模型

携带结直肠癌和胃癌异种移植肿瘤的裸鼠模型

给药剂量

每日150 mg/kg(Trifluridine和Tipiracil Hydrochloride联合用药);口服给药;每日2次,持续14天

实验结果

在结直肠癌(HCT116和SW-48细胞)和胃癌(SC-2和MKN74细胞)小鼠中,联合使用TAS-102(由Trifluridine和Tipiracil Hydrochloride组成)和Oxaliplatin在肿瘤生长抑制活性和RTV5方面显著优于单一治疗。在体内,TAS-102单一治疗能作用于MKN74/5FU细胞。TAS-102与Oxaliplatin联合用药显著增强其抗肿瘤活性。与单一治疗相比,上述联合用药不会导致显著的体重下降或毒性。

其它注意事项

请于室内测试所有化合物的溶解度。虽然化合物的实际溶解度可能与其理论值略有不同,但仍处于实验系统误差的允许范围内。

References:

[1]. 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.

生物活性

Description Tipiracil hydrochloride是一种胸苷磷酸化酶抑制剂。
靶点 thymidine phosphorylase          
IC50            

质量控制

化学结构

Tipiracil hydrochloride