CT7439 is a CDK12/13/Cyclin-K degrader, which potently inhibits the cellular activity of CDK12/13. CDK12/13 is implicated in multiple cancer types including breast, ovarian and Ewing's Sarcoma.
Our CDK12/13 inhibitor/Cyclin-K degrader has two modes of action. The compound acts as an inhibitor of CDK12 but also as a 'glue degrader' of Cyclin-K, which is the obligate co-factor for CDK12/13. This 'double punch' significantly increases the potency of the compound and leads to the inhibition of DNA repair at the transcriptional level.
CDK12/13 regulates gene transcription through the activation of RNA Polymerase II. Our molecule inhibits CDK12/13 activity and the DNA damage response (DDR) pathway in cancer cells. As such, it has the potential to synergise with other agents targeting DDR such as the PARP inhibitors.
CDK12/13 is increasingly becoming a target of interest for biopharmaceutical companies. While other companies are developing covalent and non-covalent molecules, our molecule uniquely demonstrates Cyclin-K degradation with nM potency and has good oral bioavailability.