RO-4584820

RO-4584820 is an orally bioavailable small molecule inhibitor of cyclin-dependent kinases (CDKs), primarily targeting CDK1, CDK2, and CDK4 with high potency. It acts as an ATP-competitive inhibitor and has demonstrated antineoplastic activity in preclinical models by inhibiting tumor cell proliferation across a range of human cancer cell lines. The compound was developed for the treatment of solid tumors and advanced neoplasms but has not been approved for clinical use. Its mechanism involves blocking the phosphorylation of retinoblastoma protein in tumors at efficacious exposures. Developed by Roche, it reached Phase 1 clinical trials but further development appears to have been discontinued[1][2][3][4][5][7].

Other names

CDK Inhibitor R547