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 = 35 nM),用于癌症研究。


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| 产品名称 | Phosphorylase ↓ ↑ | 其他靶点 | 纯度 | ||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Tipiracil HCl | ✔ | 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 |
|
| 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 | 279.12 |
| SMILES Code | O=C1NC(C(Cl)=C(CN2C(CCC2)=N)N1)=O.[H]Cl |
| 别名 | Tipiracil HCl; MA-1 hydrochloride; TPI; Tipiracil (hydrochloride) |
| 运输 | 蓝冰 |
| InChI Key | KGHYQYACJRXCAT-UHFFFAOYSA-N |
| Pubchem ID | 9903778 |
| 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
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