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TAS-102 结构式

TAS-102

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货号 :BCP28532CAS号 :733030-01-8纯度:98%
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  • 基本信息与产品描述
CAS号 733030-01-8 货号 BCP28532
关联产品 183204-74-2(替吡嘧啶) 183204-72-0(盐酸替吡嘧啶) 70-00-8(曲氟胸苷)
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;
SMILES
化学名称
分子式 C29H34Cl2F6N8O12 分子量 871.5
纯度 98% 配送 惯例下常温包邮
产品描述 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.
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