丙脒腙
| 中文名称 | 丙脒腙 |
|---|---|
| 中文同义词 | 丙双脒腙;丙酮双脒腙;米托胍腙(又名盐酸丙脒腙);米托瓜酮;2,2'-(丙烷-1,2-二基亚基)双(肼甲脒) |
| 英文名称 | Mitoguazone |
| 英文同义词 | 1,1'-((methylethanediylidene)dinitrilo)di-guanidin;1,1'-((methylethanediylidene)dinitrilo)diguanidine;2,2'-(1-methyl-1,2-ethanediylidene)bis-hydrazinecarboximidamid;methyl-g;methyl-gag;2,2'-(1-Methyl-1,2-ethanediylidene)bis(hydrazinecarbimidamide);Me-GAG;MGBG |
| CAS号 | 459-86-9 |
| 分子式 | C5H12N8 |
| 分子量 | 184.2 |
| EINECS号 | 202-958-7 |
| 相关类别 | 无机物;化工原料;原料;原料药 |
| Mol文件 | 459-86-9.mol |
| 结构式 |  |
丙脒腙 性质
| 熔点 | 225 °C (decomp) |
|---|---|
| 沸点 | 323.8±25.0 °C(Predicted) |
| 密度 | 1.55±0.1 g/cm3(Predicted) |
| 储存条件 | Store at -20°C |
| 酸度系数(pKa) | 7.63, 9.05(at 25℃) |
| 形态 | 固体 |
| 颜色 | 浅棕色至棕色 |
| 水溶解性 | Water: 50 mg/mL (271.44 mM; ultrasonic and adjust pH to 9 with HCl) |
| CAS 数据库 | 459-86-9 |
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.
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.
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.