cdk-4/6-in-2

CDK4/6-IN-2 is a potent inhibitor of CDK4 and CDK6 [IC50s: 2.7 and 16 nM].

CDK4/6-IN-23 (Compound 42) is a potent and selective inhibitor of CDK4/6, displaying an IC50 of 11 nM for CDK6. This compound significantly activates immune cells and enhances IL-3 production. In mice undergoing 5-FU chemotherapy, CDK4/6-IN-23 demonstrates dual bone marrow protection and immunomodulatory effects.

CDK4/6-IN-24 (Compound A) is an inhibitor of CDK4/6 with broad-spectrum antitumor activity. It can effectively inhibit various cancer cells, exhibiting an IC50 in the submicromolar range.

CDK4/6-IN-20 (Compound II-5) is an inhibitor targeting CDK4 and CDK6, exhibiting IC 50 values of 1.9 and 14.2 nM, respectively. Additionally, it suppresses cell proliferation and is applicable in cancer research.

CDK4/6-IN-21 maleate (compound I-52) is a potent inhibitor of CDK4 and CDK6, with IC50 values of 3.88 nM and 3.31 nM, respectively. This compound exhibits antitumor activity.

CDK4/6-IN-22 (Compound 1-A) is a dual inhibitor of CDK4 and CDK6.

VEGFR-2-IN-69 (Compound 5A) is an inhibitor of VEGFR-2 and telomerase (Telomerase) that enhances the expression of caspase 3, caspase 8, and caspase 9, while reducing the levels of CDK-2, CDK-4, and CDK-6. It has an IC50 of 15.46 µM against HCT116.

LSN3106729 hydrochloride, the metabolite of Abemaciclib , is a CDK inhibitor with antitumor activity. LSN3106729 hydrochloride and a CRBN ligand have been used to design PROTAC CDK4/6 degrader[1]. [1]. Edward S. Kim, et al. Abemaciclib in Combination with Single-Agent Options in Patients with Stage IV Non-Small Cell Lung Cancer: A Phase Ib Study. [2]. Nathanael Gray, et al. Degradation of cyclin-dependent kinase 4/6 (cdk4/6) by conjugation of cdk4/6 inhibitors with e3 ligase ligand and methods of use. WO2017185031A1.

CDK4/6-IN-14 is a potent, highly selective inhibitor of Cyclin-Dependent Kinases 4 and 6 (CDK4/6), with inhibition concentrations (IC50s) of 10 nM and 16 nM, respectively. It shows over 60-fold selectivity for CDK4/6 compared to CDKs 1, 2, 7, and 9, and exhibits significant selectivity against 205 other kinases.