交换名片

Tegafur | 替加氟

MCE 国际站：Tegafur

中文名：替加氟

CAS：17902-23-7

品牌：MedChemExpress (MCE)

存储条件：4°C, protect from light

生物活性：Tegafur (FT 207; NSC 148958) 是一种用于治疗癌症的化疗性 5-FU 前药；是替加氟尿嘧啶的成分。 IC50 和目标：核苷抗代谢物/类似物体外 Tegafur 被肝微粒体细胞色素 P450 酶生物活化为 5-FU。 5-FU 随后在细胞内转化为其活性代谢物 5-氟-脱氧尿苷-单磷酸 (FdUMP) 和 5-氟尿苷-三磷酸 (FUTP)；这些代谢物抑制胸苷酸合酶并嵌入 RNA，导致胸苷合成减少、DNA 合成减少、RNA 功能中断和肿瘤细胞细胞毒性。

体外：替加氟被肝微粒体细胞色素 P450 酶生物活化为 5-FU。 5-FU 随后在细胞内转化为其活性代谢物 5-氟-脱氧尿苷-单磷酸 (FdUMP) 和 5-氟尿苷-三磷酸 (FUTP)；这些代谢物抑制胸苷酸合酶并嵌入 RNA，导致胸苷合成减少、DNA 合成减少、RNA 功能中断和肿瘤细胞细胞毒性。

研究领域：Cell Cycle/DNA Damage

作用靶点：Nucleoside Antimetabolite/Analog

参考文献：
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[3]. Gabriel N. Hortobagyi, William Heim, Laura Hutchins, et al. A phase 2 study of a fixed combination of uracil ａnd ftorafur (UFT) ａnd leucovorin given orally in a 3-times-daily regimen to treat patients with recurrent metastatic breast cancer. Cancer. 2010, 116(6): 1440-1445.
[4]. K. Fujita, H. Nakayama, W. Ichikawa, et al. Pharmacokinetics of 5-Fluorouracil in Elderly Japanese Patients with Cancer Treated with S-1 (a Combination of Tegafur ａnd Dihydropyrimidine Dehydrogenase Inhibitor 5-Chloro-2,4-dihydroxypyridine). Drug Metab Dispos. 2009 Jul;37(7):1375-7. doi: 10.1124/dmd.109.027052. Epub 2009 Apr 23.
[5]. Tegafur-uracil