米托瓜酮 T35617

Product Introduction
Bioactivity


英文名: Mitoguazone

描述: Mitoguazone (Methyl-GAG) 是一种可透过血脑屏障的选择性的 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 是一种具有抗肿瘤活性的合成多羰基衍生物，可抑制 HIV DNA 整合到单核细胞和巨噬细胞中的细胞 DNA 中，诱导细胞凋亡 (apoptosis)。Mitoguazone 具可用于预防急性白血病，霍奇金淋巴瘤和非霍奇金淋巴瘤。

体外活性: 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].

体内活性: 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].

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

溶解度: H2O : 50 mg/mL (271.44 mM)


关键字: Mitoguazone

相关产品: Eugenol | Mezigdomide | KT5823 | PARP-2-IN-3 | PF-4989216 | BI 2536 | BAY 11-7082 | LY2857785 | Indirubin | Sanguinarine

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途