Cladribine

2-CdATP的核苷类似物和前药形式；对静息或增殖淋巴细胞有细胞毒性；在1和10µM浓度下抑制RNA合成并诱导静息人外周血淋巴细胞中的DNA链断裂；以浓度依赖性方式诱导U266、RPMI-8226和MM.1S多发性骨髓瘤细胞在G1期细胞周期停滞和凋亡；在12mg/kg浓度下降低HT-29结肠癌、RL淋巴瘤和RPMI-8226多发性骨髓瘤小鼠异种移植模型中的肿瘤生长A nucleoside analog and prodrug form of 2-CdATP; is cytotoxic to resting or proliferating lymphocytes; inhibits RNA synthesis and induces DNA strand breaks in resting human peripheral blood lymphocytes at 1 and 10 µM; induces cell cycle arrest at the G1 phase and apoptosis in U266, RPMI-8226, and MM.1S multiple myeloma cells in a concentration-dependent manner; reduces tumor growth in HT-29 colon cancer, RL lymphoma, and RPMI-8226 multiple myeloma mouse xenograft models at 12 mg/kg.