RGB-286638,  free base

RGB-286638 is a potent and selective cyclin-dependent kinase (CDK) inhibitor with IC₅₀ values of 1, 2, 3 and 44 nM for CDK9, CDK1, CDK2, and CDK4, respectively.  Less potent against cyclin H-CDK7 and cyclin D3-CDK6. It inhibits cell cycle progression in cancer cells by targeting CDKs, and is also found to induce apoptosis. In a range of pre-clinical models of solid and hematological tumors, RGB-286638 treatment results in tumor regression and increased survival.