Doxifluridine-d₃  (Synonyms: 去氧氟尿苷-d₃; Ro 21-9738-d₃; 5-Fluoro-5'-deoxyuridine-d₃; 5'-DFUR-d₃)

Doxifluridine-d₃ is deuterated labeled Doxifluridine (HY-B0021). Doxifluridine has anticancer activity. Doxifluidine is a 5-FU prodrug. Doxifluridine is a thymidine synthase inhibitor. Doxifluridine can enhance tumor inhibition by synergizing with a variety of drugs^[1][2][3].

氢、碳和其他元素的稳定重同位素已被纳入药物分子中，主要作为药物开发过程中定量的示踪剂。氘化引起了人们的关注，因为它可能影响药物的药代动力学和代谢谱^[1]。
Doxifluridine (1-10 μM) 在 FU-MMT-1 细胞中通过显著抑制 VEGF 的表达来抑制血管生成^[2]。
Doxifluridine (1-100 μM) 在 FU-MMT-1 细胞中低剂量时 (1 μM) 轻微增加 TSP-1 的表达，在高剂量 (100 μM) 时抑制 TSP -1 的表达^[2]。
Doxifluridine (100 μM) 在 HUVEC 细胞中能够抑制细胞增殖^[2]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Doxifluridine (61.55 mg/kg; 灌胃给药; 单剂量) 在 BALB ? cA Jcl-nu 小鼠中具有抗癌活性，且与 TNP-470 (HY-101932) 与联合用药能够显著增强抗癌活性^[2]。
Doxifluridine (200 mg/kg; 腹腔注射; 单剂量) 在 DMH 诱导的结肠癌小鼠中可以抑制胸腺嘧啶酸合酶的活性^[3]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

249.21

C₉H₈D₃FN₂O₅

3094-09-5

去氧氟尿苷-d₃；可弗-d₃

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019 Feb;53(2):211-216.  [Content Brief]

  [2]. Naganuma Y, et al. Metronomic doxifluridine chemotherapy combined with the anti-angiogenic agent TNP-470 inhibits the growth of human uterine carcinosarcoma xenografts. Cancer Sci. 2011 Aug;102(8):1545-52.  [Content Brief]

  [3]. Berne M, et al. Inhibition of thymidylate synthase after administration of doxifluridine in a transplantable colon carcinoma in the rat. Cancer Invest. 1988;6(4):377-83.  [Content Brief]

  [4]. Di Bartolomeo M, et al. Integrated treatment with doxifluridine and radiotherapy in recurrent or primary unresectable rectal cancer. A feasibility study. Tumori. 1999 May-Jun;85(3):211-3.  [Content Brief]