CDK4/6-IN-3 is a brain-penetrant CDK4/CDK6 inhibitor with Kis of <0.3 nM and 2.2 nM, respectively. CDK4/6-IN-3 inhibits CDK1 with a Ki of 110 nM. CDK4/6-IN-3 can be used for the treatment of glioblastoma[1]. CDK4|0.3 nM (Ki)|CDK6|2.2 nM (Ki)|CDK1|110 nM (Ki)
CDK4/6-IN-3 (Compound 24) inhibits MCF7 and BT549 cell lines proliferation with EC50s of 30 nM and 2.1 μM, respectively[1].
[1]. Bronner SM, et al. Design of a brain-penetrant CDK4/6 inhibitor for glioblastoma. Bioorg Med Chem Lett. 2019 Aug 15;29(16):2294-2301.