| abstract |
A preparation method for a dual-drug-linker of an ADC and a use thereof. Specifically provided are a dual-drug link assembly unit represented by formula III, or a stereoisomer thereof, or an optical isomer thereof. The dual-drug link assembly unit can be linked to a targeting linker to obtain a dual-drug targeting linker-drug conjugate represented by formula I. The specific structure can effectively reduce the aggregation of the dual-drug targeting linker-drug conjugate, which facilitates process amplification, thereby improving the efficiency of the targeting effect on tumor cells, reducing the toxic and side effects on normal cells, and at the same time, effectively overcoming drug resistance and achieving a synergistic anti-tumor effect. Compared with ADC: Ds-8201 which is already on the market, the ADC provided significantly improves the inhibition effect on HER2 positive cell strains N87 and SK-BR-3d. The dual-drug link assembly unit and the dual-drug targeting linker-drug conjugate have broad application prospects in the preparation of anti-tumor drugs for prevention and/or treatment. |