Preferred Label : CDK4/6 Inhibitor PRT3645;
NCIt definition : An orally bioavailable, brain-penetrant, selective inhibitor of cyclin-dependent kinase
(CDK) types 4 (CDK4) and 6 (CDK6), with potential antineoplastic activity. Upon oral
administration, CDK4/6 inhibitor PRT3645 selectively targets and inhibits the activity
of CDK4 and CDK6, which inhibits the phosphorylation of retinoblastoma protein (Rb)
early in the G1 phase, prevents CDK-mediated G1-S-phase transition and leads to cell
cycle arrest. This suppresses DNA replication and decreases tumor cell proliferation.
CDK4 and 6 are serine/threonine kinases that are upregulated in many tumor cell types
and play a key role in the regulation of both cell cycle progression from the G1-phase
into the S-phase and tumor cell proliferation. PRT3645 is able to penetrate the brain
and could exert its activity against CNS metastases in tumors with CDK4/6 upregulation.;
Molecule name : PRT-3645; PRT 3645;
NCI Metathesaurus CUI : CL1799276;
Origin ID : C190861;
UMLS CUI : C5783962;
Semantic type(s)
- concept_is_in_subset
- has_target
