2417302-07-7

SY-5609 (CDK7-IN-3) is an orally active, highly selective, noncovalent CDK7 inhibitor with a KD of 0.065 nM. SY-5609 shows poor inhibition on CDK2 (Ki=2600 nM), CDK9 (Ki=960 nM), CDK12 (Ki=870 nM). SY-5609 induces apoptosis in tumor cells and has antitumor activity[1][2].

CDK7: 0.065 nM (Kd); CDK2: 2600 nM (Ki); CDK9: 960 nM (Ki); CDK12: 870 nM (Ki)

[1] Jason J Marineau, et al. Discovery of SY-5609: A Selective, Noncovalent Inhibitor of CDK7. J Med Chem. 2021 Nov 2. DOI:10.1021/acs.jmedchem.1c01171
[2] Michael Bradley, et al. Inhibitors of cyclin-dependent kinase 7 (cdk7). WO2020093011A1.