TAS-102

CAS No.	733030-01-8	Cat. No.	BCP28532
Name	TAS-102
Synonyms	TAS102;TAS102;Trifluridine-tipiracil hydrochloride mixture;rifluridine-tipiracil hydrochloride mixture;
Formula	C29H34Cl2F6N8O12	M. Wt	871.5

Description	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.
Related Products	183204-74-2（Tipiracil） 183204-72-0（Tipiracil HCl） 70-00-8（Trifluridine）
Pathways	Cell Cycle/DNA Damage Apoptosis Pathway
Targets	Thymidylate Synthase Antimetabolite

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