Abstract 5123: C018, a potent and selective CDK4&9 dual inhibitor

Key Points

• To evaluate the effectiveness of a CDK4 and CDK9 dual inhibitor in overcoming resistance to palbociclib in breast cancer.
• Conducted structure-activity relationship studies for CDK4 and CDK9 inhibitors.
• Utilized a molecular design platform to identify lead compounds.
• Assessed cell viability in palbociclib-sensitive and resistant MCF-7 cell lines after treatment with the dual inhibitor.
• The CDK4&9 inhibitor reduced the viability of palbociclib-sensitive and resistant MCF-7 cell lines.
• Demonstrated over 30-fold selectivity for CDK4 and over 80-fold selectivity for CDK9 compared to CDK6.
• Simultaneous inhibition of CDK4 and CDK9 showed synergistic effects in combating palbociclib resistance.

Abstract