AG-024104

AG-024104 is a CDK inhibitor with K_i values of 2.3 nM (CDK1/cyclinB), 1.8 nM (CDK2/cyclinA), and 0.67 nM (CDK4/cyclinD). AG-024104 functionally inhibits kinase activity of CDK1/cyclinB, CDK2/cyclinA, and CDK4/cyclinD. AG-024104 serves as a negative control for peripheral leukocyte toxicity studies in preclinical development^[1]. In Vitro:AG-024104 potently inhibits purified CDK1/cyclinB, CDK2/cyclinA, and CDK4/cyclinD enzymes with K_i values of 2.3 nM, 1.8 nM, and 0.67 nM, respectively^[1].
AG-024104 (4 days) inhibits HCT-116 colorectal carcinoma cell growth with an IC₅₀ of 51 nM^[1].
AG-024104 (24 h) induces cytotoxicity in human PBMCs and monkey PBLs with TC₅₀ values of 7.2 μM and 4.0 μM, respectively^[1]. In Vivo:AG-024104 (10 mg/kg; i.v.; single bolus injection over 2-3 min) does not induce significant acute suppression of peripheral white blood cell counts in male Sprague Dawley rats, with counts remaining at ~93% of pre-treatment levels 24 hours post-dose^[1].