QR-6401 (QR6401) is a highly potent, selective, oral macrocyclic CDK2 inhibitor with IC50 of 0.37 nM (CDK2/Cyclin E1).
QR-6401 exhibits good selectivity against other closely related kinases, such as CDK1, CDK4, CDK6, CDK9 and GSK3β.
QR-6401 demonstrates good intrinsic metabolic stability and acceptable plasma protein binding in different species.
QR-6401 ( twice daily through oral gavage at 50 mg/kg for 28 days) caused significant tumor growth inhibition (TGI% = 78%) in OVCAR3 ovarian cancer xenograft model, produced robust suppression of Rb phosphorylation
