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  3. Furazolidone

Furazolidone  (Synonyms: 呋喃唑酮)

目录号: HY-B1336 纯度: 99.87%
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Furazolidone 是一种单胺氧化酶 (MAO) 的抑制剂,具有抗增殖、诱导凋亡和促进分化的活性。Furazolidone 可能通过与上调肿瘤抑制蛋白 p53 的稳定性,抑制白血病融合蛋白介导的骨髓转化。Furazolidone 在急性髓系白血病 (AML) 细胞系中展现出抗白血病活性,可用于抗 AML 的研究。

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Furazolidone Chemical Structure

Furazolidone Chemical Structure

CAS No. : 67-45-8

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Other Forms of Furazolidone:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Furazolidone is a monoamine oxidase (MAO) inhibitor with antiproliferative, apoptosis-inducing and differentiation-promoting activities. Furazolidone may inhibit leukemia fusion protein-mediated bone marrow transformation by upregulating the stability of the tumor suppressor protein p53. Furazolidone exhibits anti-leukemic activity in acute myeloid leukemia (AML) cell lines and can be used for anti-AML research[1][2].

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
Vero CC50
19 μg/mL
Compound: furazolidone
Cytotoxicity against african green monkey Vero cells after 72 hrs by CellTiterGlo assay
Cytotoxicity against african green monkey Vero cells after 72 hrs by CellTiterGlo assay
[PMID: 22691154]
体外研究
(In Vitro)

Furazolidon (50 μM;在逆转录病毒转导/转化试验中) 抑制一系列白血病融合蛋白 (包括 AML1-ETO、MLL-ENL、MLL-AF9 和 R1A-RAR-RIIa) 介导的骨髓转化,并且与 AML1-ETO 转化细胞相比,对正常小鼠骨髓 c-Kit 阳性细胞显示出相对较高的 IC50[1]
Furazolidon (1-50 μM;24-72 h) 以剂量和时间依赖的方式抑制 AML 细胞系 (Kasumi-1、NB4、MolM13、MV4-11、U937 和 HL-60) 的增殖,IC50值范围为 10-20μM,同时损害白血病细胞 (Kasumi-1、NB4、MolM-13) 形成集落的能力[1]
Furazolidon (各细胞系的 IC50值;72 h) 诱导 AML 细胞 (Kasumi-1、NB4、MV4-11、MolM13) 凋亡,与载体处理的对照组 (DMSO) 相比,Kasumi-1 中 Annexin V+/7-AAD + 百分比增加 2.1 倍,NB4 中增加 1.7 倍,MV4-11 中增加 2.0 倍,MolM13 中增加 1.6 倍,但在 U937 和 HL-60 白血病细胞中没有增加凋亡的证据[1]
Furazolidon (各细胞系的 IC50值;72 h) 诱导 AML 细胞系 (Kasumi-1、NB4、MV4-11) 分化,表现为髓系分化标志物 CD11b 表达增加、出现分化特征性的形态学变化 (如颗粒出现和细胞核浓缩) 以及 Kasumi-1 和 NB4 细胞中 NBT 阳性率增加[1]
Furazolidon (各细胞系的 IC50值;72 h) 上调 AML 细胞 (Kasumi-1、NB4、MV4-11、MolM13) 中 p53 的蛋白质水平,但不上调其 mRNA 水平[1]

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

Cell Viability Assay[1]

Cell Line: Kasumi-1, NB4, MolM13, MV4-11, U937, HL-60
Concentration: 1-50 μM
Incubation Time: 24 h, 48 h, 72 h
Result: The number of viable cells in these AML cell lines decreased in a dose-and time-dependent manner when treated with Furazolidone.
The IC50 values, measured when cells were treated with Furazolidone for 72 h, ranged from 10-20 μM.
Furazolidone also compromised the ability of Kasumi-1, NB4, and MolM-13 cells to form colonies.

Apoptosis Analysis[1]

Cell Line: Kasumi-1, NB4, MV4-11, MolM13, U937, HL-60
Concentration: IC50 values for each cell line (Kasumi-1: 20 μM; NB4: 20 μM; MV4-11: 20 μM; MolM13: 15 μM; U937: 20 μM; HL-60: 10 μM)
Incubation Time: 72 h
Result: Significantly increased the apoptosis rate in Kasumi-1, NB4, MV4-11, and MolM13 cells. The %Annexin V+/7-AAD+ increased by 2.1-fold in Kasumi-1, 1.7-fold in NB4, 2.0-fold in MV4-11, and 1.6-fold in MolM13 compared with the DMSO-treated control.
There was no evidence of increased apoptosis in U937 and HL-60 cells.

Cell Cycle Analysis[1]

Cell Line: AML cell lines
Concentration: IC50 values for each cell line (Kasumi-1: 20 μM; NB4: 20 μM; MV4-11: 20 μM; MolM13: 15 μM; U937: 20 μM; HL-60: 10 μM)
Incubation Time: 24 h
Result: Did not modulate the cell-cycle distribution in AML cells, suggesting that it prolonged cell-doubling time rather than inducing cell-cycle arrest[1].

Western Blot Analysis[1]

Cell Line: Kasumi-1, NB4, MV4-11, MolM13
Concentration: IC50 values for each cell line (Kasumi-1: 20 μM; NB4: 20 μM; MV4-11: 20 μM; MolM13: 15 μM; U937: 20 μM; HL-60: 10 μM)
Incubation Time: 72 h
Result: Up-regulated the protein level of p53 in these cells, while the relative intensity of β-actin was used as a control. The relative protein levels of p53, normalized to β-actin, were 3.2 in Kasumi-1, 2.1 in NB4, 4.0 in MV4-11, and 2.7 in MolM13. qPCR: Cell Line: Kasumi-1, NB4, MV4-11, MolM13, U937, HL-60 Concentration: Predetermined IC50 value for each cell line Incubation Time: 72 h Result: Furazolidone treatment did not up-regulate the mRNA level of p53 in these AML cell lines. However, it significantly increased the p21 mRNA level in all the cell lines tested, but the impact of this increase on the anti-leukemic effects of Furazolidone was unknown[1].
Clinical Trial
分子量

225.16

Formula

C8H7N3O5

CAS 号
性状

固体

颜色

Light yellow to yellow

中文名称

呋喃唑酮;呋氮唑酮;痢特灵

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 2 years
-20°C 1 year
溶解性数据
细胞实验: 

DMSO 中的溶解度 : 5.56 mg/mL (24.69 mM; 超声助溶 (<60°C); 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

H2O 中的溶解度 : 0.67 mg/mL (2.98 mM; 超声助溶)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 4.4413 mL 22.2064 mL 44.4129 mL
5 mM 0.8883 mL 4.4413 mL 8.8826 mL
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* 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, 2 years; -20°C, 1 year。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

* 备注:如您选择水作为储备液,请稀释至工作液后,再用 0.22 μm 的滤膜过滤除菌后使用。

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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工作液所需浓度 : mg/mL
纯度 & 产品资料

纯度: 99.87%

参考文献

完整储备液配制表

* 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, 2 years; -20°C, 1 year。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
H2O / DMSO 1 mM 4.4413 mL 22.2064 mL 44.4129 mL 111.0322 mL
DMSO 5 mM 0.8883 mL 4.4413 mL 8.8826 mL 22.2064 mL
10 mM 0.4441 mL 2.2206 mL 4.4413 mL 11.1032 mL
15 mM 0.2961 mL 1.4804 mL 2.9609 mL 7.4021 mL
20 mM 0.2221 mL 1.1103 mL 2.2206 mL 5.5516 mL

* 备注:如您选择水作为储备液,请稀释至工作液后,再用 0.22 μm 的滤膜过滤除菌后使用。

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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HY-B1336
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