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Trifluridine/tipiracil hydrochloride mixture

CAS No. : 733030-01-8

MCE 站：Trifluridine/tipiracil hydrochloride mixture

产品活性：Trifluridine-tipiracil hydrochloride mixture (TAS-102) 是一种新型的口服组合药物。由基于胸苷的抗肿瘤核苷类似物，三氟胸苷和有效的胸苷磷酸化酶 (thymidine phosphorylase) 抑制剂派替西西以1比0.5比例组成。

研究领域：Cell Cycle/DNA Damage  |  Apoptosis

作用靶点：Nucleoside Antimetabolite/Analog  |  Thymidylate Synthase

In Vitro: Trifluridine-tipiracil hydrochloride mixture (TAS-102), a novel antimetabolite combination chemotherapy agent, consists of a rediscovered antimetabolite agent, trifluorothymidine (trifluridine, FTD) combined with the metabolic inhibitor of thymidine phosphorylase, tipiracil (TPI), in a 1:0.5 molar ratio. FTD is the active antitumor component of Trifluridine-tipiracil hydrochloride mixture (TAS-102); its monophosphate form inhibits thymidylate synthase, and its triphosphate form is incorporated into DNA in tumor cells. The incorporation into DNA is known to have antitumor effects, since the inhibition of thymidylate synthase caused by oral FTD rapidly disappears after the drug's elimination. When FTD is administered orally, it is rapidly degraded to its inactive form by thymidine phosphorylase in the intestines and liver (first-pass effect). Consequently, TPI is synthesized to maintain adequate plasma concentrations of orally-administered FTD and to potentiate the antitumor activity of FTD.

In Vivo: Trifluridine-tipiracil hydrochloride mixture (TAS-102) and CPT-11 is a promising treatment option for colorectal or gastric cancer. Trifluridine-tipiracil hydrochloride mixture monotherapy has a significant antitumor activity against KM12C/5-FUFU-bearing nude mice. The combination-treated (CPT-11-and Trifluridine-tipiracil hydrochloride mixture) group is significantly superior to monotherapy. FTD systemic exposure in plasma increaseS dose-dependently. The tumor growth rate and body weight gain decreaseS dose-dependently, but FTD concentrations in the DNA of tumor tissues and white blood cells increases dose-dependently. FTD inhibits colony formation of bone marrow cells in a concentration-dependent manner.

相关产品：Drug Repurposing Compound Library Plus  |  FDA-Approved Drug Library Plus  |  FDA-Approved Drug Library Mini  |  Bioactive Compound Library Plus  |  Apoptosis Compound Library  |  Cell Cycle/DNA Damage Compound Library  |  FDA-Approved Drug Library  |  Anti-Cancer Compound Library  |  Anti-Aging Compound Library  |  Drug Repurposing Compound Library  |  Reprogramming Compound Library  |  Anti-COVID-19 Compound Library  |  FDA Approved & Pharmacopeial Drug Library  |  Anti-Blood Cancer Compound Library  |  5-Fluorouracil  |  Gemcitabine  |  Decitabine  |  5-Azacytidine  |  Cytarabine  |  5-BrdU  |  Fludarabine  |  Capecitabine  |  Ganciclovir  |  Adenosine  |  Dacarbazine  |  Floxuridine  |  Carmofur  |  Raltitrexed  |  8-Azaguanine  |  Clofarabine  |  Stavudine  |  Trifluridine  |  Doxifluridine  |  Tegafur  |  Vidarabine  |  N6,N6-Dimethyladenosine  |  6-Mercaptopurine hydrate  |  Sapacitabine  |  Tipiracil  |  Nolatrexed dihydrochloride  |  Nelarabine

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