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Mitoguazone
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Mitoguazone图片
CAS NO:459-86-9
包装与价格:
包装价格(元)
10 mM * 1 mL in Water电议
5mg电议
10mg电议
50mg电议
100mg电议
200mg电议

产品名称
米托瓜酮
Methylglyoxal-bis(guanylhydrazone)
MGBG
Methyl-GAG
产品介绍
Mitoguazone (Methylglyoxal-bis(guanylhydrazone)) 是一种具有有效抗肿瘤活性的合成多羰基衍生物。Mitoguazone 是一种可透过血脑屏障的竞争性的 S-腺苷-蛋氨酸脱羧酶 (S-adenosyl-methionine decarboxylase) 抑制剂,可破坏多胺的生物合成。Mitoguazone 诱导细胞凋亡 (apoptosis),可抑制HIV DNA整合到单核细胞和巨噬细胞中的细胞 DNA 中。Mitoguazone 具可用于急性白血病,霍奇金淋巴瘤和非霍奇金淋巴瘤的研究。
生物活性

Mitoguazone (Methylglyoxal-bis(guanylhydrazone)) is a synthetic polycarbonyl derivative with potent antineoplastic activity. Mitoguazone is a brain-penetrant and competitiveS-adenosyl-methionine decarboxylase (SAMDC)inhibitor that disruptspolyamine biosynthesis. Mitoguazone induces cellapoptosis. Mitoguazone inhibitsHIVDNA 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[1][2][3][4].

体外研究
(In Vitro)

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].

体内研究
(In Vivo)

The influence of different stages of leukemia P388 on the pharmacokinetics of the antineoplastic agent Mitoguazone in mice is investigated. Independent of the tumor stage investigated, the total clearance of mitoguazone is slightly reduced reflecting a moderate increase of AUC in the serum of leukemia-bearing animals. Furthermore, in an advanced tumor stage the drug levels in kidneys, liver, spleen and serum are found to be elevated to some extent in comparison to tumor-free controls in contrast to an earlier stage of leukemia[5].

Clinical Trial
分子量

184.20

性状

Solid

Formula

C5H12N8

CAS 号

459-86-9

中文名称

米托瓜酮

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据
In Vitro: 

H2O : 50 mg/mL(271.44 mM;ultrasonic and adjust pH to 9 with HCl)

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM5.4289 mL27.1444 mL54.2888 mL
5 mM1.0858 mL5.4289 mL10.8578 mL
10 mM0.5429 mL2.7144 mL5.4289 mL
*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80℃, 6 months; -20℃, 1 month (sealed storage, away from moisture)。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: PBS

    Solubility: 4 mg/mL (21.72 mM); Clear solution; Need ultrasonic and warming and heat to 60℃

*以上所有助溶剂都可在本网站选购。