Preferred Label : Lunresertib;
NCIt synonyms : PKMYT1 Inhibitor RP-6306; (1S)-2-amino-1-(3-hydroxy-2,6-dimethylphenyl)-5,6-dimethyl-1H-Pyrrolo[2,3-b]pyridine-3-carboxamide; 1H-Pyrrolo(2,3-b)pyridine-3-carboxamide, 2-amino-1-(3-hydroxy-2,6-dimethylphenyl)-5,6-dimethyl-,
(1S)-;
NCIt definition : An orally bioavailable inhibitor of the human membrane-associated tyrosine- and threonine-specific
cdc2-inhibitory kinase (PKMYT1), with potential antineoplastic activity. Upon oral
administration, lunresertib targets, binds to and inhibits the activity of PKMYT1.
This results in the inhibition of CDK1 phosphorylation, which may promote both premature
mitosis and a prolonged mitotic arrest, and lead to the accumulation of unrepaired
DNA damage and apoptosis in susceptible tumor cells, such as CCNE1-overexpressing
tumor cells. PKMYT1 phosphorylates CDK1 specifically when CDK1 is complexed to cyclins,
which blocks progression from G2 into mitosis.;
UNII : N95U3A7N57;
CAS number : 2719793-90-3;
Molecule name : RP-6306; RP 6306;
NCI Metathesaurus CUI : CL1661991;
Origin ID : C179323;
UMLS CUI : C5908074;
Semantic type(s)
- concept_is_in_subset
- has_target
