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盐酸替吡嘧啶 /Tipiracil hydrochloride {[allProObj[0].p_purity_real_show]}

货号:A235932 同义名: Tipiracil HCl;MA-1 hydrochloride

Tipiracil hydrochloride是一种胸苷磷酸化酶 (TPase) 抑制剂,IC50 值为 35 nM,已用于转移性结直肠癌的联合治疗。

Tipiracil hydrochloride 化学结构 CAS号:183204-72-0
Tipiracil hydrochloride 化学结构
CAS号:183204-72-0
Tipiracil hydrochloride 3D分子结构
CAS号:183204-72-0
Tipiracil hydrochloride 化学结构 CAS号:183204-72-0
Tipiracil hydrochloride 3D分子结构 CAS号:183204-72-0
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Tipiracil hydrochloride 纯度/质量文件 产品仅供科研

货号:A235932 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 Phosphorylase 其他靶点 纯度
Tipiracil hydrochloride 98%
CP-91149 +++

Glycogen phosphorylase (GP), IC50: 0.13 μM

98+%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

Tipiracil hydrochloride 生物活性

靶点
  • Phosphorylase

描述 Trifluridine have been widely used for the treatment of multiple neoplasms. But trifluridine is rapidly degraded to an inactive metabolite by thymidine phosphorylase making its poor bioavailability. Tipiracil HCl, a potent and specific chemical inhibitor of thymidine phosphorylase, creates an opportunity to improve the PK properties of trifluridine. Trifluridine/tipiracil (TAS-102) is a new orally active antineoplastic agent comprised of trifluridine and tipiracil in a molar ratio of 1:0.5. Compared with trifluridine alone, the coadministration of oral trifluridine and tipiracil in mice and monkeys led to an increased bioavailability of trifluridine and a marked increase in the trifluridine area under the concentration–time curve (AUC) and maximum observed plasma concentration (Cmax). The global phase 3 RECOURSE trial showed that, compared with a placebo control, trifluridine/tipiracil increased overall survival in patients with refractory metastatic colorectal cancer by 1.8 months[3].

Tipiracil hydrochloride 参考文献

[1]Peters GJ, Bijnsdorp IV. TAS-102: more than an antimetabolite. Lancet Oncol.2012 Dec;13(12):e518-9.

[2]Yoshino T, Mizunuma N, et al. TAS-102 monotherapy for pretreated metastatic colorectal cancer: a double-blind, randomised, placebo-controlled phase 2 trial. Lancet Oncol. 2012 Oct;13(10):993-1001.

[3]A Phase 1 Study of the Pharmacokinetics of Nucleoside Analog Trifluridine and Thymidine Phosphorylase Inhibitor Tipiracil (Components of TAS-102) vs Trifluridine Alone

Tipiracil hydrochloride 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

3.58mL

0.72mL

0.36mL

17.91mL

3.58mL

1.79mL

35.83mL

7.17mL

3.58mL

Tipiracil hydrochloride 技术信息

CAS号183204-72-0
分子式C9H12Cl2N4O2
分子量 279.123
别名 Tipiracil HCl;MA-1 hydrochloride;TPI;Tipiracil (hydrochloride)
运输蓝冰
存储条件

In solvent -20°C:3-6个月-80°C:12个月

Pure form Inert atmosphere,2-8°C

溶解方案

H2O: 50 mg/mL(179.13 mM),配合低频超声助溶

动物实验配方
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