Floxuridine(Synonyms: 氟尿苷; 5-Fluorouracil 2′-deoxyriboside)

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Floxuridine (Synonyms: 氟尿苷; 5-Fluorouracil 2′-deoxyriboside) 纯度: 99.76%

Floxuridine (5-Fluorouracil 2′-deoxyriboside) 是一种嘧啶类似物,被也是一种抗肿瘤代谢物 (oncology antimetabolites)。Floxuridine 通过激活 ATM 和 ATR 检查点信号通路,在体外抑制 Poly(ADP-Ribose) polymerase 并诱导 DNA 损伤。Floxuridine 是一种非常有效的金黄色葡萄球菌感染抑制剂并且可以诱导细胞凋亡 (apoptosis)。Floxuridine 具有抗 HSVCMV 病毒的作用。

Floxuridine(Synonyms: 氟尿苷; 5-Fluorouracil 2

Floxuridine Chemical Structure

CAS No. : 50-91-9

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10 mM * 1 mL in DMSO ¥1089 In-stock
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生物活性

Floxuridine (5-Fluorouracil 2′-deoxyriboside) is a pyrimidine analog and known as an oncology antimetabolite. Floxuridine inhibits Poly(ADP-Ribose) polymerase and induces DNA damage by activating the ATM and ATR checkpoint signaling pathways in vitro. Floxuridine is a extreamly potent inhibitor for S. aureus infection and induces cell apoptosis[1][2]. Floxuridine has antiviral effects against HSV and CMV[3].

IC50 & Target[1][2][3]

DNA synthesis

 

Bacterial

 

HSV

 

CMV

 

体外研究
(In Vitro)

Floxuridine (0-25 μM; 4-24 hours) is affectd by inhibitors of PARP and its sensitivity of ovarian cancer cells is enhanced. Co-exposed to FdUrd and the PARP inhibitor markedly increases killing cell numbers when its compare to treatment alone in ovarian cancer cells[1].
Floxuridine (300 μM; 4-24 hours) increases p-Chk1 and p-Chk2 in ovarian cancer cell lines. It may induce DNA damage and activate the ATM and ATR checkpoint signaling pathways[1].
Floxuridine (0-2.5 μM; 24 hours) causes a G1/S-phase arrest and following removal of the FdUrd, the G1/S-phase-arrested cells moved synchronously through S phase and into G2/M[1].
Floxuridine is against Mueller Hinton Broth and Tryptic Soy Broth with MIC values of 0.25 μM and 0.81 μM, respectively. It also reported to be a very potent inhibitor of staphylococcal growth (MIC, 0.025–0.00313 μM)[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.

Cell Viability Assay[1]

Cell Line: Ovarian cancer cells
Concentration: 0-25 μM
Incubation Time: 4, 8, 24 hours
Result: Was potentiated the sensitivity by  PARP inhibitors.

Western Blot Analysis[1]

Cell Line: OVCAR-8 and SKOV3ip cells
Concentration: 300 μM
Incubation Time: 4, 8, 24 hours
Result: Induced phosphorylation of Chk1 and Chk2 in two ovarian cancer cell lines

Cell Cycle Analysis[1]

Cell Line: A2780, SKOV3ip, OVCAR-5, and OVCAR-3 ovarian cancer cells
Concentration: 0.5, 1.0, 1.5, 2.0, and 2.5 μM
Incubation Time: 24 hours
Result: Induced cell arrest at G1/S-phase period.

体内研究
(In Vivo)

Floxuridine  (intraperitoneal injection; 0.5-1.25 mg/kg; once per day for 7 days or single dose) is sufficient to show statistically significant protection against S. aureus infection at 0.5 mg/kg for 7 days. In addition, 1.25 mg/kg single administration of the compound shows statistically significant protection against S. aureus infection[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.

Animal Model: C57BL/6 mice injected with S. aureus[2]
Dosage: 0.5-1.25 mg/kg
Administration: once per day for 7 days or single dose
Result: Was a very potent inhibitor for S. aureus infection in vivo.

Clinical Trial

分子量

246.19

Formula

C9H11FN2O5

CAS 号

50-91-9

中文名称

氟尿苷;氟脲脱氧核苷;氟苷;5-氟去氧尿苷

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : ≥ 150 mg/mL (609.29 mM)

H2O : ≥ 50 mg/mL (203.10 mM)

* “≥” means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 4.0619 mL 20.3095 mL 40.6190 mL
5 mM 0.8124 mL 4.0619 mL 8.1238 mL
10 mM 0.4062 mL 2.0310 mL 4.0619 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。-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: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (8.45 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (8.45 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 20.8 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 ddH₂O 中,得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (8.45 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (8.45 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 20.8 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.

    请依序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (8.45 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (8.45 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 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*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]. Huehls AM, et al. Poly(ADP-Ribose) polymerase inhibition synergizes with 5-fluorodeoxyuridine but not 5-fluorouracil in ovarian cancer cells.Cancer Res. 2011 Jul 15;71(14):4944-54.

    [2]. Yeo WS, et al. The FDA-approved anti-cancer drugs, streptozotocin and floxuridine, reduce the virulence of Staphylococcus aureus.Sci Rep.  2018 Feb 6;8(1):2521.

    [3]. Langman J, et al. Floxuridine and its influence on postnatal cerebellar development. Pediatr Res. 1972 Oct;6(10):758-64.

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