Provided are an anticancer compound comprising a cleavable linker specifically activated in a tumor microenvironment, and use thereof. The anticancer compound is represented by the following formula, wherein, R1 is a normal functional group or a protection group; R2 is Ala, Thr, Val or Ile; R3 is Ala, Val or Asn; R4 is a drug group linked via a hydroxyl group or an amino group; and the general formula of the drug is R4H. The anticancer compound is only activated at a local portion of a tumor, thus avoiding the defect of immune system damage of a traditional chemotherapeutic drug, and promoting tumor immunization by removing a tumor immunosuppression cell. The anticancer compound or pharmaceutical composition thereof is jointly used with immunotherapy, thus improving the effect of treating the tumor, and effectively inhibiting tumor metastasis and osseous metastasis.
本发明提供了一种抗癌化合物及其用途,该化合物包含在肿瘤微环境中特异性激活的可裂解连接体。该抗癌化合物由下式表示,其中,R1为正常官能团或保护基;R2为Ala、Thr、Val或Ile;R3为Ala、Val或Asn;R4为通过羟基或
氨基连接的药物基团;药物通式为R4H。该抗癌化合物仅在肿瘤局部被激活,从而避免了传统化疗药物对免疫系统损伤的缺陷,并通过清除肿瘤免疫抑制细胞促进肿瘤免疫。该抗癌化合物或其药物组合物与免疫疗法联合使用,可提高治疗肿瘤的效果,有效抑制肿瘤转移和骨转移。