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TAS-102 Chemical Structure

TAS-102

Data Sheet For research use only. Not for human use.
Cat. No. :BCP28532CAS No. :733030-01-8Purity:98%
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  • Chemical Properties&Biological Activity
CAS No. 733030-01-8 Cat. No. BCP28532
Related Products 183204-74-2(Tipiracil) 183204-72-0(Tipiracil HCl) 70-00-8(Trifluridine)
Name TAS-102
Synonyms TAS102;TAS102;Trifluridine-tipiracil hydrochloride mixture;rifluridine-tipiracil hydrochloride mixture;
SMILES
Chemical Name
Formula C29H34Cl2F6N8O12 M. Wt 871.5
Purity 98% Storage Store at 4-8°C
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.
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