PRO-6E is an orally active, Cereblon ligand-based PROTAC that promotes MET degradation, achieving up to 81.9% effectiveness at a concentration of 1 μM in MKN-45 cells. It demonstrates tumor growth inhibition both in vivo and in vitro, alongside inducing cell apoptosis and cell cycle arrest. Notably, its structure comprises a Cereblon ligand (blue), a linker (black), and an ALK/c-Met inhibitor Crizotinib component (pink). [1]

PRO-6E (0.03-10 μM；48小时) 显著抑制了MKN-45、SNU-638细胞的生长[1]。在1μM浓度下，持续作用超过24小时，PRO-6E促使MKN-45细胞中的MET降解[1]。同时，PRO-6E 在0.1-1 μM浓度范围内，作用48小时后，能够显著增加MKN-45细胞G2/M期的细胞比例，而减少S期的细胞比例[1]。

PRO-6E（口服；30 mg/kg/天；连续15天）在MKN-45细胞源异种移植肿瘤模型中抑制了肿瘤生长[1]。