Fluorouracil (Adrucil).|51-21-8|(5-氟脲嘧啶; 5-FU)-陌孚医药/Medlife

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

目录号: PC15667 纯度: ≥98%

CAS No. :51-21-8

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中文名称	Fluorouracil (Adrucil).
中文别名	5-氟尿嘧啶;5-氟-2,4(1H,3H)-嘧啶二酮;5-氟脲嘧啶;双喃呋啶;氟尿嘧啶;2,4-二羟基-5-氟嘧啶;5-氟尿嘧啶,5FU;5-Fluorouracil 5-氟尿嘧啶;5氟尿嘧啶;5-氟尿嘧啶标准品;5-氟尿嘧啶(5-氟脲嘧啶);5-氟尿嘧啶,BR;氟二氧嘧啶;氟尿嘧啶（双喃呋啶）;氟脲嘧啶 EP标准品;氟脲嘧啶,5-氟脲嘧啶;氟脲嘧啶杂质混合 EP标准品;磺胺嘧啶钠;5-氟脲嘧啶,5-氟-2,4(1H,3H)-嘧啶二酮;二喃氟啶;氟胞嘧啶杂质A(EP) 标准品;氟脲嘧啶;双呋啶;双喃
英文名称	Fluorouracil (Adrucil)
英文别名	Fluorouracil;1-FLUORO-1H-PYRIMIDINE-2,4-DIONE;2,4-DIHYDROXY-5-FLUOROPYRIMIDINE;5-FLUORO-1H-PYRIMIDINE-2,4-DIONE;5-FLUORO-2,4(1H,3H)-PYRIMIDINEDIONE;5-FLUORO-2,4-DIHYDROXYPYRIMIDINE;5-fluoro-2,4-pyrimidinedione;5-FLUOROPYRIMIDINE-2,4(1H,3H)-DIONE;5-Fluoropyrimidine-2,4-dione;5-FU;[180]-5-Fluorouracil;2,4(1H,3H)-Pyrimidinedione, 5-fluoro-;2,4-dioxo-5-fluoropyrimidine;3h)-pyrimidinedione,5-fluoro-4(1h;5-faracil;5-Flouracyl;5-fluor-2,4(1h,3h)-pyrimidindion;5-Fluor-2,4-dihydroxypyrimidin;5-Fluorouracil;5-Fluorouracil (5-FU, 5-Fluoracil);Fluorouracil (5-Fluoracil, 5-FU);2,4-Dihydroxy-5-fluoropyrimidine,5-FU,5-Fluoro-2,4(1H,3H)-pyrimidinedione;2,4-Dihydroxy-5-fluoropyriMidine;5-fluoro-2,4-dioxopyrimidine;5-fluoro-uracile;Arumel;Efudex;Efudix;Efurix;Fluri;Fluril;U-8953;Ulup;Fluorouracil;5-Fluorouracil;5-Fluoro-2,4(1H,3H)-pyrimidinedione;5-Fluoro-2,4-pyrimidinedione
Cas No.	51-21-8
分子式	C₄H₃FN₂O₂
分子量	130.08
包装储存	4°C, protect from light *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

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.

性状

Solid

IC50 & Target[1][2]

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. 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.

Medlife 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.

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

运输条件

Room temperature or refrigerated transportation.

储存方式

4°C, protect from light

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

ClinicalTrial

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] [Information]

[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. [Information]

[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. [Information]

[4]. McQuade RM, et al. Gastrointestinal dysfunction and enteric neurotoxicity following treatment with anticancer chemotherapeutic agent 5-fluorouracil. Neurogastroenterol Motil. 2016 Jun 28. [Information]

[5]. Yin L, et al. Antitumor effects of oncolytic herpes simplex virus type 2 against colorectal cancer 体外研究 and in vivo. Ther Clin Risk Manag. 2017 Feb 7;13:117-130. [Information]

[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. [Information]

[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. [Information]

溶解度数据

体外研究:

DMSO : 50 mg/mL (384.38 mM; Need ultrasonic)

配制储备溶液

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

产品不同，其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液；配成溶液后，建议分装保存，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，建议在 6 个月内使用，-20°C 储存时，建议在 1 个月内使用。

体内研究:

建议根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都建议先按照 体外研究 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.

建议依照次序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.5 mg/mL (19.22 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (19.22 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH?O 中，得到澄清透明的生理盐水溶液
2.

建议依照次序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.5 mg/mL (19.22 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (19.22 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
3.

建议依照次序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.5 mg/mL (19.22 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (19.22 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。
4.

建议依照次序添加每种溶剂： 5% DMSO 40% PEG300 5% Tween-80 50% saline
Solubility: ≥ 2.5 mg/mL (19.22 mM); Clear solution
5.

建议依照次序添加每种溶剂： 5% DMSO 95% (20% SBE-β-CD in saline)
Solubility: ≥ 2.5 mg/mL (19.22 mM); Clear solution
6.

建议依照次序添加每种溶剂： 5% DMSO 95% saline
Solubility: 2.5 mg/mL (19.22 mM); Clear solution; Need ultrasonic

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产品使用指南

Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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