ds3032

Milademetan (DS-3032) 是一种具有口服活性和有效性的 MDM2 抑制剂，具有抗肿瘤活性，诱导 G1 细胞周期阻滞、衰老和凋亡。Milademetan 可用于研究急性髓系白血病和实体肿瘤。

Milademetan (DS-3032b or DS-3032) is a potent and selective MDM2 inhibitor with potential antineoplastic activity. Milademetan (p.o.) binds to and prevents the binding of MDM2 protein to the transcriptional activation domain of the tumor suppressor protei

Milademetan is a potent and selective MDM2 inhibitor. MDM2 inhibitor DS-3032b binds to and prevents the binding of MDM2 protein to the transcriptional activation domain of the tumor suppressor protein p53 upon oral administration. By preventing this MDM2-p53 interaction, the proteosome-mediated enzymatic degradation of p53 is inhibited and the transcriptional activity of p53 is restored. This results in the restoration of p53 signaling and leads to the p53-mediated induction of tumor cell apoptosis.