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A novel potent CDK4/6 inhibitor BPI-16350 in preclinical cancer models by Shuiping Gao; Ru-Jiao Liu; Yang Chen; Yi-qian Wang; Hong Chen; Hui-juan Zhang; Tian-yi Ma; Jia-bing Wang; Xi-Chun Hu; Jian Zhang is a scholarly article available to read on EtoBox.

What is A novel potent CDK4/6 inhibitor BPI-16350 in preclinical cancer models about?

## Abstract Inhibition of the cyclin-dependent kinase (CDK) 4/6-retinoblastoma (Rb) pathway is an effective therapeutic strategy against cancer. Here, we report a novel CDK4/6 inhibitor, BPI-16350, identified from comprehensive screening of a large panel of kinases. A series of investigations to evaluate anti-tumor activity show that BPI-16350 exhibits potent antiproliferative activities by inducing G1 arrest in a wide range of human Rb-positive tumor cells. Multiple carcinoma xenografts reveal that BPI-16350 has equivalent or improved anti-tumor efficacy compared with palbociclib or abemaciclib, and achieves obvious tumor regression without body weight loss in experimental animals, where pharmacokinetic study in SD rats indicates a longer half-life of BPI-16350 with once daily. Furthermore, BPI-16350 achieves excellent brain penetration with a nearly sixfold brain-to-plasma ratio in mice, suggesting the potential of treating tumor brain metastasis. Taken together, our findings indicate that BPI-16350 is a novel CDK4/6 inhibitor with favorable pharmaceutical properties as an anti-cancer agent.

Author

Shuiping Gao; Ru-Jiao Liu; Yang Chen; Yi-qian Wang; Hong Chen; Hui-juan Zhang; Tian-yi Ma; Jia-bing Wang; Xi-Chun Hu; Jian Zhang

Publisher

Research Square Platform LLC

Published

2022

Language

EN