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苯丁酸氮芥(CBL)的活性酯通过共价联接的方式与抗人直肠癌单克隆抗体5OH.19偶联,形成的免疫偶联物CBL一5OH.19具有较高的药物/抗体比率(25～30∶1)以及很好的导向活性。在体外30分钟试验和24小时试验中,CBL—50H.19对人直肠癌LoVo细胞均具有很强的体外杀伤活性.其效果比游离的CBL强。CBL—50H.19对人膀胱癌E—J细胞无杀伤活性;CBL与正常小鼠IgG偶联组成的免疫偶联物对LoVo细胞和E—J细胞均无杀伤作用。这表明CBL—50H.19对人直肠癌细胞不但具有较强的杀伤能力.而且具有好的杀伤特异性.
The active ester of chlorambucil (CBL) was conjugated to the anti-human rectal cancer monoclonal antibody 5OH.19 by covalent attachment and the resulting immunoconjugate CBL-5OH.19 had a higher drug / antibody ratio (25 ~ 30: 1) and good guiding activity. CBL-50H.19 had a strong in vitro cytotoxic activity against human rectal cancer LoVo cells in 30-minute and 24-hour in vitro tests, which was more effective than free CBL. CBL-50H.19 had no cytotoxic activity on human bladder cancer E-J cells. The immunoconjugate consisting of CBL and normal mouse IgG had no killing effect on LoVo cells and E-J cells. This indicates that CBL-50H.19 not only has strong killing ability on human rectal cancer cells, but also has good killing specificity.