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  3. Furazolidone

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[2].

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Furazolidone Chemical Structure

Furazolidone Chemical Structure

CAS No. : 67-45-8

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10 mM * 1 mL in DMSO
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Customer Review

Based on 3 publication(s) in Google Scholar

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Description

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].

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]
In Vitro

Furazolidone (50 μM; in the RTTA assay) inhibits bone marrow transformation mediated by a series of leukemia fusion proteins, including AML1-ETO, MLL-ENL, MLL-AF9, and R1A-RAR-RIIa, and shows a relatively higher IC50 value for normal murine bone-marrow c-Kit positive cells compared to AML1-ETO transformed cells[1].

Furazolidone (1-50 μM; 24 h-72 h) inhibits the proliferation of AML cell lines (Kasumi-1, NB4, MolM13, MV4-11, U937, and HL-60) in a dose-and time-dependent manner, with IC50 values ranging from 10-20 μM, and also compromises the ability of leukemic cells (Kasumi-1, NB4, MolM-13) to form colonies[1].
Furazolidone (IC50 values for each cell line; 72 h) induces apoptosis in AML cells (Kasumi-1, NB4, MV4-11, MolM13), with a 2.1-fold increase in %Annexin V+/7-AAD+ in Kasumi-1, 1.7-fold in NB4, 2.0-fold in MV4-11, and 1.6-fold in MolM13 compared with the vehicle-treated control (DMSO), but has no evidence of increased apoptosis in U937 and HL-60 leukemic cells[1].
Furazolidone (IC50 values for each cell line; 72 h) induces the differentiation of AML cell lines (Kasumi-1, NB4, MV4-11), as indicated by the increased expression of the myeloid differentiation marker CD11b, evident morphologic changes characteristic of differentiation (such as the appearance of granules and condensation of the nucleus), and an increased NBT-positive rate in Kasumi-1 and NB4 cells[1].
Furazolidone (IC50 values for each cell line; 72 h) up-regulates the protein level, but not the mRNA level, of p53 in AML cells (Kasumi-1, NB4, MV4-11, MolM13)[1].

MedChemExpress (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
Molecular Weight

225.16

Formula

C8H7N3O5

CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C1OCCN1/N=C/C2=CC=C([N+]([O-])=O)O2

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 5.56 mg/mL (24.69 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : 0.67 mg/mL (2.98 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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Purity & Documentation

Purity: 99.87%

References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 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

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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  • 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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Furazolidone
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