Darinaparsin

一种二甲基化砷与谷胱甘肽相连的抗癌活性物质；对DU145、LNCap、PC3前列腺癌细胞具有细胞毒性（IC50s分别为5-10µM）以及对患者来源的原代前列腺癌细胞（IC50s为2.5-20µM）有效，同时对Jurkat T细胞淋巴瘤和L540霍奇金淋巴瘤细胞也有作用（IC50s分别为2.7和1.3µM）；在1.5 µM下减少Gli-2的转录，而在3µM下无此效果；在DU145和PC3前列腺癌小鼠异种移植模型中，以100mg/kg每隔一天给药，减少肿瘤生长。A dimethylated arsenic linked to glutathione with anticancer activities; cytotoxic to DU145, LNCap, PC3 prostate cancer cells (IC50s = 5-10 µM) and patient-derived primary prostate cancer cells (IC50s = 2.5-20 µM), as well as Jurkat T cell lymphoma and L540 Hodgkin lymphoma cells (IC50s = 2.7 and 1.3 µM, respectively); decreases transcription of Gli-2 at 1.5 but not 3 µM; reduces tumor growth in DU145 and PC3 prostate cancer mouse xenograft models at 100 mg/kg every other day.