CDK2 degrader7 is an orally active CDK2 degrader with DC50 values of 13 nM in MKN1 cells and 17 nM in TOV21G cells. It induces G1 phase arrest in MKN1 cells and achieves tumor suppression in the HCC1569 (CCNE1 amplified) xenograft model. CDK2 degrader7 is utilized in research on CCNE1 amplification-type cancers.

CDK2:13 nM (DC50 , MKN1cells)

CDK2 degrader 7 (Compound 37) exhibits potent CDK2 degradation activity in MKN1 (CCNE1 amplified) and TOV21G (CCNE1 non-amplified) cells, with DC50 values of 13 nM and 17 nM, respectively. It shows strong antiproliferative activity against MKN1 (CCNE1 amplified) cells, with an IC50 of 9 nM, whereas it is less effective against TOV21G (CCNE1 non-amplified) cells, with an IC50 of 5760 nM. Within 72 hours, across a concentration range of 4.88-5000 nM, CDK2 degrader 7 induces maximum G1 phase arrest at 78 nM in MKN1 cells (targeted action), and non-targeted G2/M phase accumulation occurs at 2500 nM.

CDK2 degrader 7 (Compound 37) demonstrates potent antitumor activity in the HCC1569 (CCNE1-amplified) xenograft model when administered orally at doses of 10-50 mg/kg, once or twice daily for 28 days \.