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。
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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。 |
靶点 |
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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]. |
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 |
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 |