Floxuridine是一种嘧啶类似物,也是一种抗肿瘤代谢物。它抑制胸苷酸合成酶,导致 DNA 合成中断和细胞毒性。它是一种可诱导细胞凋亡的金黄色葡萄球菌感染抑制剂 ,具有抗HSV和CMV病毒的作用。
产品描述
Floxuridine is an antimetabolite, floxuridine inhibits thymidylate synthase, resulting in disruption of DNA synthesis and cytotoxicity.
体外活性
Floxuridine exhibits higher affinity for PEPT1 than the corresponding 5'-O-mono amino acid ester prodrugs. [1] Floxuridine combined with Leucovorin results in synergistic inhibitory effects on growth of human T-lymphoblast leukemia cells. [2] Floxuridine significantly inhibits the uptake of both [(3)H]-inosine and [(3)H]-adenosine (60-70% of control), while its amino acid ester prodrugs including Val, Phe, Pro, Asp, and Lys esters exhibits markedly decreased inhibition potency (10-30% of control). [3] Floxuridine inhibits cell proliferation by more than 50% relative to the untreated control cells at 36 days, the cell numbers still increases fourfold compared with the initial cell density. Floxuridine results in prolonged effects on the proliferation of human Tenon's capsule fibroblasts in vitro. [4] Floxuridine (FUDR) is an ideal drug for hepatic arterial infusion (HAI) due to its short half life, steep dose response curve, high total body clearance, and high hepatic extraction. [5]
Cas No.
50-91-9
分子式
C9H11FN2O5
分子量
246.194
别名
FUDR;Deoxyfluorouridine;氟尿苷;5-Fluorouracil 2'-deoxyriboside;NSC 27640
储存和溶解度
DMSO:24.6 mg/mL (100 mM)
H2O:24.6 mg/mL (100 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years