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Mitoguazone

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Chemical Structure| 459-86-9 同义名 : Methylglyoxal-bis(guanylhydrazone);MGBG;Methyl-GAG
CAS号 : 459-86-9
货号 : A995052
分子式 : C5H12N8
纯度 : 97%
分子量 : 184.202
MDL号 : MFCD00067519
存储条件:

粉末 Keep in dark place,Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月

溶解度 :

DMSO: 7 mg/mL(38 mM),配合低频超声,并水浴加热至45℃助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

H2O: 50 mg/mL(271.44 mM),配合低频超声,并调节pH至9

动物实验配方:
生物活性
描述 Mitoguazone, also known as Methylglyoxal-bis(guanylhydrazone), is a synthetic polycarbony derivative with potent antitumour activity. Mitoguazone is a brain-permeable, competitive inhibitor of SAMDC, which disrupts polyamine biosynthesis. Mitoguazone induces apoptosis. Mitoguazone inhibits the integration of HIV DNA into the cellular DNA of monocytes and macrophages. Mitoguazone has therapeutic potential for acute leukaemia, Hodgkin's lymphoma and non-Hodgkin's lymphoma[1][2][3][4].At concentrations as low as 0.5 μg/mL, Mitoguazone competitively inhibits spermine synthesis in lymphocytes. At concentrations of 30 μg/mL or higher, Mitoguazone inhibits protein synthesis and mitochondrial respiration[1].Mitoguazone induces apoptosis in Burkitt's lymphoma cell lines (Raji, Ramos and Daudi) and prostate carcinoma cell line (MPC 3), with apoptosis correlating with concentration and time, and induces p53-independent programmed cell death in human breast cancer MCF7 cell line[2].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

5.43mL

1.09mL

0.54mL

27.14mL

5.43mL

2.71mL

54.29mL

10.86mL

5.43mL

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.

[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.