NCIt definition : An orally bioavailable diaminopyrimidine compound and a cyclin-dependent kinase (CDK)
inhibitor with potential antineoplastic activity. CDKs are ATP-dependent serine/threonine
kinases that are important regulators of cell cycle progression and are frequently
overexpressed in cancerous cells. R547 selectively binds to and inhibits CDKs, especially
CDK1/cyclin B, CDK2/cyclin E, and CDK4/cyclin D1. The inhibition of CDKs results in
cell cycle arrest, inhibition of tumor cell proliferation, and induction of apoptosis.
By inhibiting CDK activity, R547 also reduces phosphorylation of the retinoblastoma
(Rb) protein, thereby preventing activation of transcription factor E2F and leading
to further suppression of tumor cell proliferation.;
UNII : T61871RKRI;
InChIKey : JRNJNYBQQYBCLE-UHFFFAOYSA-N;
CAS number : 741713-40-6;
Molecule name : R547; RO-4584820; RO 4584820; R 547;