Voreloxin Hydrochloride 是一种新型拓扑异构酶 II 抑制剂，能够诱导 DNA 双链断裂，阻滞 G2 期，最终细胞凋亡。

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

Voreloxin potentially inhibits the relaxation of topoisomerase II relaxation with IC50 of 3.2 μg /mL with no effect on topoisomerase II cleavage. Voreloxin has a cytotoxic activity against human tumor cell lines more potent than that of etoposide. [1] Voreloxin also has broad anti-proliferative activity in 15 cell lines, including 4 drug-resistant lines, with IC50 ranging from 0.04 to 1.155 μM. [2]

Voreloxin (50 mg/kg i.p.) shows potent antitumor activity in mice implanted with P388 leukemia cells. [1] Voreloxin (25 mg/kg i.v.) demonstrates strong tumor growth inhibition in 10 of 11 solid tumor (ovarian, breast, melanoma, gastric, colon, and lung) xenograft models, 2 hematologic tumor xenograft models, 3 multidrug resistant tumor models and 3 murine syngeneic tumor models (Colon 26, M5076 Ovarian Sarcoma, Lewis Lung carcinoma). [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.

175519-16-1

C18H20ClN5O4S

437.9

Vosaroxin;SNS-595 hydrochloride;(3S-反式)-1,4-二氢-7-[3-甲氧基-4-(甲基氨基)-1-吡咯烷基]-4-氧代-1-(2-噻唑基)-1,8-萘啶-3-羧酸单盐酸盐

DMSO:20 mg/ml (45.67 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years