フラゾリドン
Based on 3 publication(s) in Google Scholar
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
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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 99.87%
- CAS 番号: 67-45-8
- 分子式: C8H7N3O5
- 分子量:225.16
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
MedChemExpress(MCE)の使用を引用している文献 Furazolidone
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生物活性
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Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| THP-1 | IC50 |
>100 μM
Compound: FZD
|
Cytotoxicity against human THP-1 cells assessed as inhibition of cell growth incubated for 48 hrs by resazurin dye based assay
Cytotoxicity against human THP-1 cells assessed as inhibition of cell growth incubated for 48 hrs by resazurin dye based assay
|
[PMID: 36516584] |
| THP-1 | IC50 |
>100 μM
Compound: FZD
|
Cytotoxicity against human THP-1 cells assessed as inhibition of cell growth incubated for 72 hrs by resazurin staining based analysis
Cytotoxicity against human THP-1 cells assessed as inhibition of cell growth incubated for 72 hrs by resazurin staining based analysis
|
[PMID: 37859713] |
| 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] |
| Vero | IC50 |
>100 μM
Compound: FZD
|
Cytotoxicity against African green monkey Vero cells assessed as inhibition of cell growth incubated for 48 hrs by resazurin dye based assay
Cytotoxicity against African green monkey Vero cells assessed as inhibition of cell growth incubated for 48 hrs by resazurin dye based assay
|
[PMID: 36516584] |
| Vero | IC50 |
>100 μM
Compound: FZD
|
Cytotoxicity against African green monkey Vero cells assessed as inhibition of cell growth incubated for 48 hrs by resazurin staining based analysis
Cytotoxicity against African green monkey Vero cells assessed as inhibition of cell growth incubated for 48 hrs by resazurin staining based analysis
|
[PMID: 37859713] |
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.
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Cell Line:Kasumi-1, NB4, MolM13, MV4-11, U937, HL-60
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Concentration:1-50 μM
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Incubation Time:24 h, 48 h, 72 h
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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.
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Cell Line:Kasumi-1, NB4, MV4-11, MolM13, U937, HL-60
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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)
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Incubation Time:72 h
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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.
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Cell Line:AML cell lines
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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)
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Incubation Time:24 h
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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].
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Cell Line:Kasumi-1, NB4, MV4-11, MolM13
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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)
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Incubation Time:72 h
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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].
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 67-45-8
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性状 Solid
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分子量 225.16
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分子式 C8H7N3O5
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Color Light yellow to yellow
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SMILES
O=C1OCCN1/N=C/C2=CC=C([N+]([O-])=O)O2
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別名
Furazolidone
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (3)
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Journal Impact Factor
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Most Recent
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Zebrafish
Ronidazole Is a Superior Prodrug to Metronidazole for Nitroreductase-Mediated Hepatocytes Ablation in Zebrafish Larvae. [Abstract]2023 Jun;20(3):95-102. PMID: 37229597 -
Heliyon
Furazolidone reduces the pathogenesis of Trueperella pyogenes and Pseudomonas aeruginosa co-infection in a mouse model. [Abstract]2024 Oct 19;10(20):e39629. PMID: 39506932 -
溶剤 & 溶解度
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)
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.
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.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
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データシート (281 KB)
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SDS (419 KB)
- English - EN (419 KB)
- Français - FR (419 KB)
- Deutsch - DE (419 KB)
- Norwegian - NO (419 KB)
- Español - ES (419 KB)
- Swedish - SV (419 KB)
- Italian - IT (419 KB)
- Korean - KR (419 KB)
- Portuguese - PT (419 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Jiang X, et al. A novel application of furazolidone: anti-leukemic activity in acute myeloid leukemia. PLoS One. 2013 Aug 9;8 (8) :e72335. [Content Brief]
[2]. Ma S, et al. Furazolidone Increases Survival of Mice Exposed to Lethal Total Body Irradiation through the Antiapoptosis and Antiautophagy Mechanism. Oxid Med Cell Longev. 2021 Feb 4;2021:6610726. [Content Brief]
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.