Mitoguazone
Based on 6 publication(s) in Google Scholar
Mitoguazone (Methylglyoxal-bis(guanylhydrazone)) is a synthetic polycarbonyl derivative with potent antineoplastic activity. Mitoguazone is a brain-penetrant and competitive S-adenosyl-methionine decarboxylase (SAMDC) inhibitor that disrupts polyamine biosynthesis. Mitoguazone induces cell apoptosis. Mitoguazone inhibits HIV DNA integration into the cellular DNA in both monocytes and macrophages. Mitoguazone has the potential for acute leukemia, Hodgkin's and non-Hodgkin's lymphoma treatment.
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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: 99.23%
- CAS 番号: 459-86-9
- 分子式: C5H12N8
- 分子量:184.20
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保管条件:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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MedChemExpress（MCE）の使用を引用している文献 Mitoguazone
More
生物活性
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO | IC50 |
3.3 μM
Compound: MGBG
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Cytotoxicity against CHO cells expressing MGBG polyamine transporter after 48 hrs by MTT assay
Cytotoxicity against CHO cells expressing MGBG polyamine transporter after 48 hrs by MTT assay
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[PMID: 20064676] |
| CHO-MG | IC50 |
>100 μM
Compound: MGBG
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Cytotoxicity against MGBG polyamine transporter deficient CHO-MG cells after 48 hrs by MTT assay
Cytotoxicity against MGBG polyamine transporter deficient CHO-MG cells after 48 hrs by MTT assay
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[PMID: 20064676] |
| T-24 | IC50 |
1.1 μM
Compound: MGBG
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Antiproliferative activity against human T24 bladder carcinoma cells
Antiproliferative activity against human T24 bladder carcinoma cells
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[PMID: 8421290] |
Mitoguazone competitively inhibits spermidine synthesis in lymphocytes at concentrations as low as 0.5 μg/mL. Levels of 30 μg/mL or more inhibit protein synthesis and mitochondrial respiration[1].
The ability of Mitoguazone to induce apoptosis by inhibiting the polyamine pathway is assessed in three Burkitt's lymphoma cell lines (Raji, Ramos and Daudi) and one prostate carcinoma cell line (MPC 3). Mitoguazone induces apoptosis in all the different human cancer cell lines tested in a concentration- and time-dependent way, and triggers a p53-independent programmed cell death in the human breast cancer MCF7 cell line[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 459-86-9
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性状 Solid
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分子量 184.20
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分子式 C5H12N8
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Color Light brown to brown
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SMILES
CC(/C=N/NC(N)=N)=N\NC(N)=N
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別名
Methylglyoxal-bis(guanylhydrazone); MGBG; Methyl-GAG
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (6)
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Journal Impact Factor
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Most Recent
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Cardiovasc Diabetol
Dysregulated Rbfox2 produces aberrant splicing of CaV1.2 calcium channel in diabetes-induced cardiac hypertrophy. [Abstract]2023 Jul 6;22(1):168. PMID: 37415128 -
Mar Drugs
Spermine Promotes the Formation of Conchosporangia in Pyropia haitanensis Through Superoxide Anions. [Abstract]2025 Jul 30;23(8):309. PMID: 40863626 -
bioRxiv
ATP13A2 Loss of Function-Driven Polyamine Dysregulation Induces SAM Depletion and Epigenetic Astrocyte Toxicity. [Abstract]2026 Apr 6:2026.04.02.716164. PMID: 41993310 -
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溶剤 & 溶解度
H2O : 50 mg/mL (271.44 mM; ultrasonic and adjust pH to 9 with HCl)
DMSO : 5.83 mg/mL (31.65 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)
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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* 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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* 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)
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: PBS
Solubility: 4 mg/mL (21.72 mM); Clear solution; Need ultrasonic and warming and heat to 60°C
純度とドキュメンテーション
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データシート (272 KB)
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SDS (394 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. J Rizzo, et al. Pharmacokinetic Profile of Mitoguazone (MGBG) in Patients With AIDS Related non-Hodgkin's Lymphoma. Invest New Drugs. 1996;14(2):227-34. [Content Brief]
[2]. K Davidson, et al. Mitoguazone Induces Apoptosis via a p53-independent Mechanism. Anticancer Drugs. 1998 Aug;9(7):635-40. [Content Brief]
[3]. Xia Jin, et al. Inhibition of HIV Expression and Integration in Macrophages by Methylglyoxal-Bis-Guanylhydrazone. J Virol. 2015 Nov;89(22):11176-89. [Content Brief]
[4]. A M Levine, et al. Mitoguazone Therapy in Patients With Refractory or Relapsed AIDS-related Lymphoma: Results From a Multicenter Phase II Trial. J Clin Oncol. 1997 Mar;15(3):1094-103. [Content Brief]
[5]. R Amlacher, et al. Influence of Leukemia P388 on the Pharmacokinetics of Mitoguazone in B6D2F1 Mice. Pharmazie. 1990 May;45(5):364-6. [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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO / H2O | 1 mM | 5.4289 mL | 27.1444 mL | 54.2888 mL | 135.7220 mL |
| 5 mM | 1.0858 mL | 5.4289 mL | 10.8578 mL | 27.1444 mL | |
| 10 mM | 0.5429 mL | 2.7144 mL | 5.4289 mL | 13.5722 mL | |
| 15 mM | 0.3619 mL | 1.8096 mL | 3.6193 mL | 9.0481 mL | |
| 20 mM | 0.2714 mL | 1.3572 mL | 2.7144 mL | 6.7861 mL | |
| 25 mM | 0.2172 mL | 1.0858 mL | 2.1716 mL | 5.4289 mL | |
| 30 mM | 0.1810 mL | 0.9048 mL | 1.8096 mL | 4.5241 mL | |
| H2O | 40 mM | 0.1357 mL | 0.6786 mL | 1.3572 mL | 3.3931 mL |
| 50 mM | 0.1086 mL | 0.5429 mL | 1.0858 mL | 2.7144 mL | |
| 60 mM | 0.0905 mL | 0.4524 mL | 0.9048 mL | 2.2620 mL | |
| 80 mM | 0.0679 mL | 0.3393 mL | 0.6786 mL | 1.6965 mL | |
| 100 mM | 0.0543 mL | 0.2714 mL | 0.5429 mL | 1.3572 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.
Mitoguazone 関連分類
HY-106634 関連分類
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