CT7001, a Novel Orally Bio-Available CDK7 Inhibitor, Is Highly Active in in-Vitro and in-Vivo Models of AML

CDK7 is considered an important new target for the treatment of human cancer as it controls the activity of key enzymes involved in cell cycle progression, including other cyclin dependent kinases such as CDK1, CDK2, CDK4 and CDK6. As a master regulator of transcription CDK7 also promotes the expression of key oncogenes such as c-Myc through the phosphorylation of Rpb1 subunit of RNA polymerase II.

Both transcription and cell cycle regulation are dysregulated in Acute Myeloid Leukaemia (AML) (Shafer and Grant 2016). Here, we investigated the therapeutic potential of CT7001 (ICEC0942), a novel orally bio-available ATP competitive CDK7 inhibitor (Hazel et al. 2017), in pre-clinical AML models.