Vosaroxin

拓扑异构酶II抑制剂；诱导超螺旋DNA松弛(IC50=3.2µg/ml)；以浓度依赖性方式诱导CCRF-CEM细胞中的DNA双链断裂和A549细胞中的细胞周期停滞在G2期；抑制15种癌细胞系的增殖，包括对阿霉素、依托泊苷或顺铂有耐药性的癌细胞(IC50s=0.04-1.15µM)；以20mg/kg的剂量抑制多药耐药SBC-3/ETP或PC-14/CDDP小鼠异种移植模型中的肿瘤生长。A topoisomerase II inhibitor; induces relaxation of supercoiled DNA (IC50 = 3.2 µg/ml); induces DNA double-strand breaks in CCRF-CEM cells and cell cycle arrest at the G2 phase in A549 cells in a concentration-dependent manner; inhibits proliferation in a panel of 15 cancer cell lines, including cancer cells resistant to doxorubicin, etoposide, or cisplatin (IC50s = 0.04-1.15 µM); inhibits tumor growth in multidrug-resistant SBC-3/ETP or PC-14/CDDP mouse xenograft models at 20 mg/kg.分子式C18H19N5O4S分子量401.4O=C1C2=CC=C(N3C[C@H](NC)[C@@H](OC)C3)N=C2N(C4=NC=CS4)C=C1C(O)=O