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编 号:F401730
分子式:C6H4N2O2
分子量:136.11
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10mM*1mL in DMSO
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5mg
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10mg
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50mg
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生物活性:
Eniluracil (5-Ethynyluracil) is an orally active dihydropyrimidine dehydrogenase (DPD) inhibitor. Eniluracil irreversibly inhibits DPD, increases the oral bioavailability of 5-fluorouracil to 100%, and facilitates the uniform absorption and toxicity of 5-fluorouracil. Eniluracil can be used in cancer research of combination with fluoropyrimidines (including 5-fluorouracil). Eniluracil is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

体内研究:
Eniluracil (5-Ethynyluracil) (1 mg/kg; i.p.; single daily for 3 days) exhibits neither toxicity nor intrinsic antitumor activity, and greatly improves FUra (5-fluorouracil) therapy in rats.Animal Model:Female Fischer 344/HSD rats (6 to 7-week-old; 150-200 g).
Dosage:1 mg/kg
Administration:Intraperitoneal injection; single daily for 3 days (l h before FUra (5-fluorouracil) and for an additional 2 days after FUra therapy)
Result:Produced complete tumor regression that was sustained for at least 90 days posttherapy when combined with 3.5 mg/kg FUra, however, 35 mg/kg FUra alone produced partial responses in 75% of the treated animals ( the tumors regrew in all of these animals).
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