Tipiracil HCl
产品说明书
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同义名 : | Tipiracil HCl; MA-1 hydrochloride; TPI; Tipiracil (hydrochloride) |
| CAS号 : | 183204-72-0 | |
| 货号 : | A235932 | |
| 分子式 : | C9H12Cl2N4O2 | |
| 纯度 : | 98% | |
| 分子量 : | 279.12 | |
| MDL号 : | - | |
| 存储条件： |
Pure form Inert atmosphere, 2-8°C In solvent -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : |
H2O: 50 mg/mL(179.13 mM)，配合低频超声助溶 |
| 生物活性 | |||
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| 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]. | ||
| 实验方案 | |||
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| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
3.58mL 0.72mL 0.36mL |
17.91mL 3.58mL 1.79mL |
35.83mL 7.17mL 3.58mL |
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