Synonyms: (Rac)-RP-6306
Compound class:
Synthetic organic
Comment: Lunresertib (RP-6306) is the first lead candidate in the class of protein kinase, membrane associated tyrosine/threonine 1 (PKMYT1) inhibitors to be advanced for clinical evaluation [3]. It is orally bioavailable and selective for PKMYT1, and it is active in appropriate preclinical xenograft models of solid tumours [1]. PKMYT1 is a negative regulator of CDK1 [2], and its inhibition induces activation of CDK1 selectively in CCNE1-overexpressing cells; CCNE1 being a chromosome 19q12 locus that is amplified in multiple tumour types and which is a marker of poor prognosis and/or insensitivity to cytotoxic oncotherapies. As a monotherapy lunresertib induces synthetic lethality in combination with CCNE1 amplification (or alongside inactivating mutations in FBXW7 and PPP2R1A).
Structure note: the INN record for lunresertib does not specify the (S) stereo specification that is declared in the original disclosure of RP-6306's chemical structure [3]. We depict the racaemic mixture with no defined stereo centers. |
|
Classification | |
Compound class | Synthetic organic |
IUPAC Name |
2-amino-1-(3-hydroxy-2,6-dimethylphenyl)-5,6-dimethylpyrrolo[2,3-b]pyridine-3-carboxamide |
International Nonproprietary Names | |
INN number | INN |
13035 | lunresertib |
Synonyms |
(Rac)-RP-6306 |
Database Links | |
BindingDB Ligand | 50598851 |
CAS Registry No. | 2719793-90-3 (source: WHO INN record) |
ChEMBL Ligand | CHEMBL5199076 |
GtoPdb PubChem SID | 491299993 |
PubChem CID | 156869388 |
RCSB PDB Ligand | QGI |
Search Google for chemical match using the InChIKey | ARBRHWRTXPWZGN-UHFFFAOYSA-N |
Search Google for chemicals with the same backbone | ARBRHWRTXPWZGN |
Search PubMed clinical trials | lunresertib |
Search PubMed titles | lunresertib |
Search PubMed titles/abstracts | lunresertib |
UniChem Compound Search for chemical match using the InChIKey | ARBRHWRTXPWZGN-UHFFFAOYSA-N |
UniChem Connectivity Search for chemical match using the InChIKey | ARBRHWRTXPWZGN-UHFFFAOYSA-N |