MS140 is a specific and highly potent CDK4/6 kinase inhibitor and also a CDK4/6 degrader (PROTAC).
MS140 potently and selectively both inhibits and degrades CDK4/6 kinases in CDK4/6i-S tumor cells by targeting them to the CRL4–CRBN–E3 ubiquitin complex.[1]
Treatment of mice with MS140 promoted degradation of CDK4/6 kinases and suppression of RB–E2F output in JeKo-1 (MCL) and Colo25 (colorectal carcinoma) xenografts in vivo.[1]
[1] Xuewei Wu, et al. Nature Cancer volume 2, pages429–443 (2021)