TAS-102
| CAS号 | 733030-01-8 | 货号 | BCP28532 |
| 中文名 | TAS-102 | ||
| 英文名 | TAS-102 | ||
| 中文别名 | |||
| 英文别名 | TAS102;TAS102;Trifluridine-tipiracil hydrochloride mixture;rifluridine-tipiracil hydrochloride mixture; | ||
| 分子式 | C29H34Cl2F6N8O12 | 分子量 | 871.5 |
| 生物活性 | TAS-102 is an investigational drug candidate for metastatic colorectal cancer. It contains trifluridine (TFT) and Tipiracil hydrochloride (TTP) in a molar ratio of 1;0.5. Trifluridine is a nucleoside analog, and tipiracil hydrochloride is a thymidine phosphorylase inhibitor, which prevents rapid metabolism of trifluiridine, increasing the bioavailability of trifluiridine. After oral administration of TAS-102, TFT is phosphorylated to the active monophosphate form TF-TMP, which binds covalently to the active site of thymidylate synthase, thereby reducing the nucleotide pool levels required for DNA replication. Furthermore, the triphosphate form TF-TTP can be incorporated into DNA, which induces DNA fragmentation and leads to the inhibition of tumor growth. TPI exhibits a dual effect: 1) an anti-angiogenic effect mediated through the inhibition of thymidine phosphorylase, which plays an important role in nucleotide metabolism and a variety of development processes, including angiogenesis, 2) increased bioavailability of the normally short-lived antimetabolite TFT by preventing its degradation into the inactive form trifluorothymine (TF-Thy). The synergistic effect of the components in TAS-102 may demonstrate antitumor activity in 5-FU-resistant cancer cells. | ||
| 上下游产品 | 183204-74-2（替吡嘧啶） 183204-72-0（盐酸替吡嘧啶） 70-00-8（曲氟胸苷） | ||
| 信号通路 | Cell Cycle/DNA Damage Apoptosis Pathway | ||
| 靶 点 | Thymidylate Synthase Antimetabolite | ||
结构式
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