Iobenguane sulfate 是一种具有抗肿瘤活性的神经递质去甲肾上腺素的类似物。Iobenguane sulfate 是一种高亲和力的霍乱毒素底物,干扰细胞单核(ADP-核糖基化)。放射性碘代 Iobenguane sulfate 可用于肾上腺肿瘤诊断和肿瘤靶向药物的研究。
产品描述
Iobenguane sulfate is a high-affinity substrate for cholera toxin that interferes with cellular mono(ADP-ribosylation). Radioiodinated Iobenguane sulfate is clinically used as a tumor-targeted radiopharmaceutical in the diagnosis and treatment of adrenergic tumors.
体外活性
Iobenguane sulfate is an effective effector of endogenous mono(ADP-ribosyl) transferases of turkey and human erythrocyte membranes, exerting its effect in the μM concentration range. Iobenguane sulfate (2-20 μg/ml; 72 hours) suppresses cell growth in a panel of human and mouse leukemia, melanoma, fibrosarcoma, and neuroblastoma cell lines.
体内活性
Iobenguane sulfate (20 mg/kg; i.p.; daily on days 3-6) displays antitumor activity. Iobenguane sulfate testes for its toxicity on male strain AF (N1Ell5) mice with 5 daily injections. At 50 mg/kg body weight, all animals died after 1-4 doses and 4/16 animals died on a schedule of 44 mg/kg. The survival of male strain AF mice inoculates with N1E115 neuroblastoma and treats according to NIH protocols for new drug testing with 9 daily injections of Iobenguane sulfate (40 mg/kg), Marking prolongation of survival but no cures were observed.
Cas No.
87862-25-7
分子式
C16H22I2N6O4S
分子量
648.26
别名
硫酸碘苄胍 EP标准品;MIBG sulfate;Iobenguane sulfate
储存和溶解度
DMSO:100 mg/mL (308.52 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years