CPD-10 is a potent CCND1 and CDK4 PROTAC degrader. CPD-10 exhibits anti-proliferative effects on tumor cells and can also induce apoptosis. CPD-10 can be used for the study of breast cancer and lung cancer [1]. (Pink: Cdk4/cyclin D1 ligand; Blue: Ligands for E3 Ligase ligand; Black: linker ).
In Vivo, CPD-10 (oral administration; 10 mg/kg) has an oral bioavailability of 15% after 12 hours[1].
In Vitro, CPD-10 (1 nM-10 μM; 3-6 days) exhibits anti-proliferative activity against Calu-1, MCF7 and T47D cells, with IC50 values of 1.7, 16.6 and 17.5 nM respectively[1]. CPD-10 (3.9-1000 nM; 48 h) can reduce the expression levels of CCND1, CCND3, CDK4, FoxM1, Cyclin A2 and p-Rb proteins in T47D cells[1]. CPD-10 (15-200 nM; 6 days) can induce apoptosis in T47D cells[1]. CPD-10 (1 nM-10 μM; 3-6 days) has a half-maximal inhibitory concentration (IC50) of 19.5 nM against parental T47D cells and an IC50 of 33 nM against Palbociclib -resistant T47D cells[1].
References:
[1]. Jing Liu, et al. Compounds and methods of treating cancers. French, WO2024183798A1.
In Vivo, CPD-10 (oral administration; 10 mg/kg) has an oral bioavailability of 15% after 12 hours[1].
In Vitro, CPD-10 (1 nM-10 μM; 3-6 days) exhibits anti-proliferative activity against Calu-1, MCF7 and T47D cells, with IC50 values of 1.7, 16.6 and 17.5 nM respectively[1]. CPD-10 (3.9-1000 nM; 48 h) can reduce the expression levels of CCND1, CCND3, CDK4, FoxM1, Cyclin A2 and p-Rb proteins in T47D cells[1]. CPD-10 (15-200 nM; 6 days) can induce apoptosis in T47D cells[1]. CPD-10 (1 nM-10 μM; 3-6 days) has a half-maximal inhibitory concentration (IC50) of 19.5 nM against parental T47D cells and an IC50 of 33 nM against Palbociclib -resistant T47D cells[1].
References:
[1]. Jing Liu, et al. Compounds and methods of treating cancers. French, WO2024183798A1.