Antibody-coupled drug intermediate SET0582 as well as preparation method and application thereof

The invention relates to an antibody coupled drug intermediate SET0582 and a preparation method and application thereof, the intermediate SET0582 has the following structure: # imgabs0, the intermediate SET0582 is subjected to fixed-point coupling of SN38 to an antibody through a dimethyl bromo-quin...

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Bibliographische Detailangaben
Hauptverfasser: LI HAIHONG, JIA ZHONGQUAN, ZHAO YONGSHENG, ZHENG XINGWANG, ZHANG WENMENG
Format: Patent
Sprache:chi ; eng
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Zusammenfassung:The invention relates to an antibody coupled drug intermediate SET0582 and a preparation method and application thereof, the intermediate SET0582 has the following structure: # imgabs0, the intermediate SET0582 is subjected to fixed-point coupling of SN38 to an antibody through a dimethyl bromo-quinoxaline active reaction group, an ADC coupled drug intermediate with a DAR value of 4 is obtained, the homogeneity of an ADC drug can be improved, and the stability of the antibody can be improved; after the medicine enters the body, the linker with peg and VC fragments can improve the solubility and metabolic distribution of the medicine. 本发明涉及一种抗体偶联药物中间体SET0582及制备方法与应用,中间体SET0582具有如下结构:#imgabs0#该中间体SET0582,通过二甲基溴代喹恶啉活性反应基团将SN38定点偶联到抗体上,得到DAR值为4的ADC偶联药物中间体,可以提高ADC药物的均一性,可以提高抗体的稳定性;药物进入体内后,具有peg和VC片段的Linker,可以提高药物的溶解性和代谢分布。