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Mitoguazone

Catalog No. T35617 CAS 459-86-9

Synonyms: MGBG, Methyl-GAG

Mitoguazone (Methyl-GAG) is a selective S-adenosyl-methionine decarboxylase inhibitor that penetrates the blood-brain barrier and disrupts polyamine biosynthesis. Mitoguazone is a synthetic polycarbonyl derivative with anti-tumor activity that inhibits the integration of HIV DNA into cellular DNA in monocytes and macrophages, inducing apoptosis. Mitoguazone can be used to prevent acute leukemia, Hodgkin lymphoma and non-Hodgkin lymphoma.

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Mitoguazone, CAS 459-86-9

Pack Size	Availability	Price/USD
2 mg	In stock	$ 68.00
5 mg	5 days	$ 119.00
10 mg	5 days	$ 178.00
25 mg	5 days	$ 323.00
50 mg	5 days	$ 491.00
100 mg	6-8 weeks	$ 718.00
500 mg	5 days	$ 1,470.00

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Biological Description

Chemical Properties

Storage & Solubility Information

Description	Mitoguazone (Methyl-GAG) is a selective S-adenosyl-methionine decarboxylase inhibitor that penetrates the blood-brain barrier and disrupts polyamine biosynthesis. Mitoguazone is a synthetic polycarbonyl derivative with anti-tumor activity that inhibits the integration of HIV DNA into cellular DNA in monocytes and macrophages, inducing apoptosis. Mitoguazone can be used to prevent acute leukemia, Hodgkin lymphoma and non-Hodgkin lymphoma.
In vitro	At concentrations as low as 0.5 μg/mL, Mitoguazone competitively inhibits spermidine synthesis in lymphocytes. At levels of 30 μg/mL or higher, it inhibits protein synthesis and mitochondrial respiration[5]. The ability of Mitoguazone to induce apoptosis by inhibiting the polyamine pathway was evaluated in three Burkitt lymphoma cell lines (Raji, Ramos, and Daudi) and a prostate cancer cell line (MPC 3). Mitoguazone induces apoptosis in a concentration- and time-dependent manner in all tested human cancer cell lines, and triggers p53-independent programmed cell death in the human breast cancer MCF7 cell line[2].
In vivo	The impact of different stages of leukemia (P388) on the pharmacokinetics of the anti-tumor drug Mitoguazone was investigated in mice. Regardless of the tumor stage under study, there was a slight reduction in the total clearance rate of Mitoguazone, reflecting a moderate increase in the AUC in the serum of leukemia-afflicted animals. Additionally, at the late tumor stage, the drug levels in the kidneys, liver, spleen, and serum were somewhat higher compared to early-stage leukemia, and were elevated to a certain extent compared to the tumor-free control[1].

Synonyms	MGBG, Methyl-GAG
Molecular Weight	184.2
Formula	C5H12N8
CAS No.	459-86-9

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

H2O: 50 mg/mL (271.44 mM), when pH is adjusted to 9 with HCl. Sonication is recommended.

References and Literature

1. R Amlacher, et al. Influence of Leukemia P388 on the Pharmacokinetics of Mitoguazone in B6D2F1 Mice. Pharmazie. 1990 May;45(5):364-6. 2. K Davidson, et al. Mitoguazone Induces Apoptosis via a p53-independent Mechanism. Anticancer Drugs. 1998 Aug;9(7):635-40. 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. 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. 5. 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.

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Keywords

Mitoguazone 459-86-9 Apoptosis Microbiology/Virology Proteases/Proteasome HIV Protease MGBG Methyl-GAG inhibitor inhibit

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