RGNCY-0009 (CDK2-4 Inhibitor)

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Cancer is characterized by the uncontrolled proliferation of cells. The biochemical processes which control a cell’s progression though the cell cycle are critical to this process. The cyclin dependent kinases CDK4 and CDK6 are key regulators of the transition though G1 phase. RGNCY-0009 is a potent inhibitor of CDK 2 (IC50 = 0.159uM) and CDK4 (IC50 = 0.0038uM) in addition to activity against ARK5, FGFR1, PDGFRb, and PI3K-d. RGNCY-0009 has demonstrated a GI50 of 0.025 uM for both Granta-519 and mantle cell lymphoma cell lines.

Systematic Name: 8-cyclopentyl-2-((4-(4-methylpiperazin-1-yl)phenyl)amino)-7-oxo-7,8-dihydropyrido[2,3-d]pyrimidine-6-carbonitrile


Molecular Weight: 429.52

Formula: C24H27N7O

PMID: 24417566

Reference: Reddy, MV Ramana, et al. "Discovery of 8-Cyclopentyl-2-[4-(4-methyl-piperazin-1-yl)-phenylamino]-7-oxo-7, 8-dihydro-pyrido [2, 3-d] pyrimidine-6-carbonitrile (7x) as a Potent Inhibitor of Cyclin-Dependent Kinase 4 (CDK4) and AMPK-Related Kinase 5 (ARK5)." Journal of Medicinal Chemistry 57.3 (2014): 578-599.

Tags: CDK4, CDK2, Cancer, lymphoma, RGNCY-0009, ARK5, FGFR1, PDGFRb, PI3K-d