| CAS |
No.51-21-8 |
| 中文名称 |
5-氟尿嘧啶(10mM in DMSO,无菌） |
| 英文名称 |
5-Fluorouracil(10mM in DMSO，Sterile） |
| 分子式 |
C4H3FN2O2 |
| 分子量 |
130.08 |
| 溶解性 |
请根据自己的实验要求使用。 |
| 外观(性状) |
无菌溶液 |
| 储存条件 |
Stroe at -20℃，6 months. |
| 靶点 |
DNA/RNA Synthesis |
| 通路 |
Cell Cycle;DNA Damage/DNA Repair |
| 背景说明 |
5-Fluorouracil具有抗肿瘤活性。是一种尿嘧啶的类似物 (nucleoside antimetabolite/analog)，可以通过抑制胸苷酸合成酶影响嘧啶的合成。 |
| 生物活性 |
5-Fluorouracil (5-FU) is an analogue of uracil and a potent antitumor agent. 5-Fluorouracil affects pyrimidine synthesis by inhibiting thymidylate synthetase thus depleting intracellular dTTP pools. 5-Fluorouracil induces apoptosis and can be used as a chemical sensitizer. 5-Fluorouracil also inhibits HIV.[1-7] |
| In Vitro |
5-Fluorouracil (5-Fu) 和 NSC 123127 (Dox) 具有协同抗癌功效。5-Fu/Dox-DNM 对人乳腺癌 (MDA-MB-231) 细胞的 IC50 值为 0.25 μg/mL，细胞毒性分别增加 11.2 倍和 6.1 倍分别为 Dox-DNM 和 5-Fu-DNM[1]。在 5-Fluorouracil (5-FU) 和 CDDP 处理的 NFBD1 抑制 NPC 细胞中，使用慢病毒介导的短发夹 RNA 耗尽 NPC CNE1 细胞系中的 NFBD1 表达，并且这些细胞的敏感性升高。NFBD1 敲低导致 CDDP 或 5-FU 处理的 CNE1 细胞明显诱导细胞凋亡[2]。 |
| In Vivo |
5-Fluorouracil (23 mg/kg，每周 3 次) 持续 14 天，在处理开始后第 3 天诱导与急性肠道炎症相关的胃肠道传输加速，这可能导致第 7 天后观察到的 ENS 持续变化和 14 项处理导致胃肠道传输延迟和结肠运动障碍[4]。 |
| 动物实验 |
Mice receive intraperitoneal injections of 5-FU (23 mg/kg)， 3 times a week via a 26 gauge needle. 5-FU is dissolved in 100% dimethyl sulfoxide (DMSO) to make 1 M/L stock solution refrigerated at ?20°C. The stock is then defrosted and diluted with sterile water to make 0.1 M/L (10% DMSO) solutions for intraperitoneal injections. The dose of 5-FU is calculated to be equivalent to standard human dose per body surface area. The low doses of 5-FU (10-40 mg/kg) have been shown to have antitumor efficacy in mouse models of cancer. Sham-treated mice received 10% DMSO in sterile water via intraperitoneal injection three times a week via a 26 gauge needle. The injected volumes are calculated to the body weight; the maximum volume does not exceed 200 μL per injection. Mice are euthanized via cervical dislocation at 3 (2 treatments)， 7 (3 treatments)， and 14 (6 treatments) days after the first injection and colon is collected for in vitro experiments. |
| 数据来源文献 |
[1]. Han R， et al. Amphiphilic dendritic nanomicelle-mediated co-delivery of 5-fluorouracil and NSC 123127 for enhanced therapeutic efficacy. J Drug Target. 2016 Jun 29:1-28. [Epub ahead of print]
[2]. Zeng Q， et al. Knockdown of NFBD1/MDC1 enhances chemosensitivity to NSC 119875 or 5-fluorouracil in nasopharyngeal carcinoma CNE1 cells. Mol Cell Biochem. 2016 Jul;418(1-2):137-46.
[3]. Jones DH， et al. Ten-Year and Beyond Follow-up After Treatment With Highly Purified Liquid-Injectable Silicone for HIV-Associated Facial Lipoatrophy: A Report of 164 Patients. Dermatol Surg. 2019 Jul;45(7):941-948.
[4]. McQuade RM， et al. Gastrointestinal dysfunction and enteric neurotoxicity following treatment with anticancer chemotherapeutic agent 5-fluorouracil. Neurogastroenterol Motil. 2016 Jun 28.
[5]. Yin L， et al. Antitumor effects of oncolytic herpes simplex virus type 2 against colorectal cancer in vitro and in vivo. Ther Clin Risk Manag. 2017 Feb 7;13:117-130.
[6]. Snyder SM， et al. Initial Experience with Topical Fluorouracil for Treatment of HIV-Associated Anal Intraepithelial Neoplasia. J Int Assoc Physicians AIDS Care (Chic). 2011;10(2):83-88.
[7]. Pek Yee Lum， et al. Discovering modes of action for therapeutic compounds using a genome-wide screen of yeast heterozygotes. Cell. 2004 Jan 9;116(1):121-37. |
| 规格 |
0.1ml 0.3ml 0.5ml 1ml 1.5ml |
| 单位 |
瓶 |
中文
英语
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