CDK2 degrader 8 is a selective cyclin-dependent kinase 2 ( CDK2 ) degrader. CDK2 degrader 8 can be used in studies related to CDK2 degradation and HR + HER2 - breast cancer [1].
In Vivo, CDK2 degrader 8 (compound 1) (100 mg/kg; i.p.; once daily for 21 days) inhibits tumor growth in the HR+ HER2- xMCF-7 human breast cancer xenograft model in female BALB/c nude mice, and achieves 50% TGI on day 21[1].
In Vitro, CDK2 degrader 8 (compound 1) induces CDK2 degradation in CDK2-HiBiT HEK293 cells after 24 h of treatment, with a Dmax of 64.8%. In the corresponding GSPT1 Live-cell HiBiT assay, the Dmax of GSPT1 is only 3.3%, demonstrating selectivity for CDK2 degradation[1]. CDK2 degrader 8 (1 μM; 60 min) exhibits a CLint of 46.6 μL/min/mg in the human liver microsome stability assay[1].
References:
[1]. WO 2025/181261 A1. Cyclopropyl and 1,3,4-oxadiazole compounds that mediate protein degradation and methods of use thereof. Published September 4, 2025.
In Vivo, CDK2 degrader 8 (compound 1) (100 mg/kg; i.p.; once daily for 21 days) inhibits tumor growth in the HR+ HER2- xMCF-7 human breast cancer xenograft model in female BALB/c nude mice, and achieves 50% TGI on day 21[1].
In Vitro, CDK2 degrader 8 (compound 1) induces CDK2 degradation in CDK2-HiBiT HEK293 cells after 24 h of treatment, with a Dmax of 64.8%. In the corresponding GSPT1 Live-cell HiBiT assay, the Dmax of GSPT1 is only 3.3%, demonstrating selectivity for CDK2 degradation[1]. CDK2 degrader 8 (1 μM; 60 min) exhibits a CLint of 46.6 μL/min/mg in the human liver microsome stability assay[1].
References:
[1]. WO 2025/181261 A1. Cyclopropyl and 1,3,4-oxadiazole compounds that mediate protein degradation and methods of use thereof. Published September 4, 2025.