A first-in-class CDK4 inhibitor demonstrates in vitro, ex-vivo and in vivo efficacy against ovarian cancer

Laychiluh Bantie,Solomon Tadesse,Jimma Likisa,Mingfeng Yu,Benjamin Noll,Gary Heinemann,Noor A Lokman,Carmela Ricciardelli,Martin K Oehler,Andrew Beck,Rupal Pradhan,Robert Milne,Hugo Albrecht,Shudong Wang

Gynecologic Oncology（2020）

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摘要

•CDDD2–94 is the most selective CDK4 inhibitor identified to date.•CDDD2–94 has potent anti-proliferative activity against panel of cancer cell lines.•CDDD2–94 provides the proof-of-concept that selectivity towards CDK4 over CDK6 reduces the bone marrow toxicity.•CDDD2–94 exhibits robust anti-tumor efficacy against ovarian cancer xenografts.•CDDD2–94 synergises with an mTOR inhibitor against ovarian cancer.

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关键词

Cyclin-dependent kinases,CDK4 inhibitor,Ovarian cancer,Drug discovery and development,Palbociclib

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