5-Fluorouracil(Synonyms: 5-氟脲嘧啶; 5-FU)

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5-Fluorouracil (Synonyms: 5-氟脲嘧啶; 5-FU) 纯度: 99.67%

5-Fluorouracil (5-FU) 是一种尿嘧啶的类似物 (nucleoside antimetabolite/analog),是一种有效的抗肿瘤药。5-Fluorouracil 通过抑制胸苷酸合成酶影响嘧啶的合成,从而耗尽细胞内dTTP 池。5-Fluorouracil 诱导细胞凋亡 (apoptosis),可用作化学敏化剂。5-Fluorouracil 还可抑制 HIV 病毒。5-Fluorouracil (5-FU) 可破坏外泌体特异性的 rRNA。

5-Fluorouracil(Synonyms: 5-氟脲嘧啶; 5-FU)

5-Fluorouracil Chemical Structure

CAS No. : 51-21-8

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10 mM * 1 mL in DMSO ¥500 In-stock
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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[1][2]. 5-Fluorouracil also inhibits HIV[3].

IC50 & Target[1][6]

Human Endogenous Metabolite

 

HIV

 

体外研究
(In Vitro)

5-Fluorouracil (5-Fu) and NSC 123127 (Dox) show synergistic anticancer efficacy. The IC50 value of 5-Fu/Dox-DNM toward human breast cancer (MDA-MB-231) cells is 0.25 μg/mL, presenting an 11.2-fold and 6.1-fold increase in cytotoxicity compared to Dox-DNM and 5-Fu-DNM, respectively[1]. In 5-fluorouracil (5-FU) and CDDP treated NFBD1-inhibited NPC cells, the NFBD1 expression in NPC CNE1 cell lines is depleted using lentivirus-mediated short hairpin RNA, and the sensitivity of these cells is elevated. NFBD1 knockdown leads to an obvious induction of apoptosis in CDDP- or 5-FU-treated CNE1 cells[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

5-Fluorouracil (23 mg/kg, 3 times/week) for 14 days, induces accelerated gastrointestinal transit associated with acute intestinal inflammation at day 3 after the start of treatment, which may have led to persistent changes in the ENS observed after days 7 and 14 of treatment contributing to delayed gastrointestinal transit and colonic dysmotility[4].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

分子量

130.08

Formula

C4H3FN2O2

CAS 号

51-21-8

中文名称

5-氟脲嘧啶;双喃呋啶

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

溶解性数据
In Vitro: 

DMSO : 100 mg/mL (768.76 mM; Need ultrasonic)

H2O : 20 mg/mL (153.75 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 7.6876 mL 38.4379 mL 76.8758 mL
5 mM 1.5375 mL 7.6876 mL 15.3752 mL
10 mM 0.7688 mL 3.8438 mL 7.6876 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (protect from light)。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 5% DMSO    40% PEG300    5% Tween-80    50% saline

    Solubility: ≥ 2.5 mg/mL (19.22 mM); Clear solution

  • 2.

    请依序添加每种溶剂: 5% DMSO    95% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (19.22 mM); Clear solution

  • 3.

    请依序添加每种溶剂: 5% DMSO   95% saline

    Solubility: 2.5 mg/mL (19.22 mM); Clear solution; Need ultrasonic

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献
  • [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.

Animal Administration
[2]

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.

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

参考文献
  • [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.

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