CDK12/13 Inhibitor :: Carrick Therapeutics, Inc.

CT7439: CDK12/13 inhibitor/Cyclin-K Degrader

Implicated in many types of cancer

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.

One molecule, two distinct mechanisms

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.

Regulating gene transcription

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.

View CDK12/13 Biology Schematic

First-in-class and best-in-class opportunity

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.