LAI, KATHARINE C.,赖 凯萨琳 C,賴 凱薩琳 C,W HERBST, ROBERT W.,贺伯斯特 罗伯特,賀伯斯特 羅伯特,HILDERBRAND, SCOTT ALAN,希德布兰德 史考特 艾伦,希德布蘭德 史考特 艾倫
申请号：
TW106103674
公开号：
TW201731532A
申请日:
2017.02.03
申请国别(地区):
TW
年份:
2017
代理人:
摘要：
The present invention provides a novel method for preparing a cell-binding agent cytotoxic agent conjugate. The method comprises the step of reacting a cell-binding agent with a cytotoxic agent or a cytotoxic agent-linker compound having a reactive group capable of forming a covalent bond with the cell-binding agent at a pH between 4 to 9 in the presence of a buffer solution with high ionic strength, wherein the cell-binding agent comprises a lysine ε-NH2 group that forms a covalent bond with the cytotoxic agent or the cytotoxic agent-linker compound having an amine-reactive group. The cell-binding agent-cytotoxic agent conjugates prepared according to the methods described herein are also included in the present invention.本發明提供一種製備細胞結合劑-細胞毒性劑結合物之新穎方法。該方法包括以下步驟:使細胞結合劑與具有能夠與細胞結合劑形成共價鍵之反應基團的細胞毒性劑或細胞毒性劑-連接子化合物在4至9之間的pH值下在具有高離子強度之緩衝溶液存在下反應,其中該細胞結合劑包含與具有胺反應基團之細胞毒性劑或細胞毒性劑-連接子化合物形成共價鍵之離胺酸ε-NH2。本發明亦包括根據本文中描述之方法製備的細胞結合劑-細胞毒性劑結合物。
