Voreloxin hydrochloride (SNS-595 hydrochloride) is a potent inhibitor of Topoisomerase II with broad-spectrum anti-tumor activity.

Voreloxin可能通过抑制topoisomerase II的松弛作用来发挥其作用，其IC50为3.2 μg/mL，对topoisomerase II的切割作用无影响。Voreloxin对人类肿瘤细胞系的细胞毒性活性强于etoposide。[1] 此外，Voreloxin在15种细胞系中展示了广泛的抗增殖活性，包括4种耐药细胞系，IC50范围从0.04到1.155 μM。[2]

Voreloxin（50 mg/kg i.p.）在植入P388白血病细胞的小鼠中展现出强大的抗肿瘤活性。[1] Voreloxin（25 mg/kg i.v.）在11种实体瘤（卵巢、乳腺、黑色素瘤、胃、结肠和肺）异种移植模型中的10种、2种血液肿瘤异种移植模型、3种多药耐药肿瘤模型以及3种小鼠同源肿瘤模型（Colon 26, M5076卵巢肉瘤, Lewis肺癌）中显示出强烈的肿瘤生长抑制作用。[2]

Cell lines: P388 leukemia cells. Concentrations: about 10 μg/mL. Incubation Time: 72 hours. Method: Cells are seed in a 96-well microtiter plate (0.1 mL/well), preincubated for 24 h except for P388 cells, and incubated with various concentrations of a test compound in the 5% CO2 incubator at 37℃ for 72 h. Then, 0.02 mL MTT solution (5 mg/mL) is added in each well, and a further 4 h cells culturing is carried out. The medium is removed and 0.2 mL of DMSO is added in each well to dissolve the formed formazan. The absorbance is measured using Multiskan Bichromatic.

Animal Models: Mice implanted with P388 leukemia cells. Dosages: about 50 mg/kg. Administration: i.p.