- Guide to PHARMACOLOGY
Synonyms: RGB 286638 | RGB286638
Compound class: Synthetic organic
Comment: RGB-286638 is a multi-targeted kinase inhibitor. It inhibits transcriptional-type CDKs (cyclin dependent kinases) such as CDK9, to achieve an anti-multiple myeloma effect which is independent of p53 status , providing a proof of concept which could lead to the development of compounds with activity in p53 deleted multiple myeloma.
A Phase I safety and tolerability study, NCT01168882, was withdrawn from ClinicalTrials.gov (2012), although results of this study have been published..
Ligand Activity Visualisation Charts
These are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts.✖
1. Cirstea D, Hideshima T, Santo L, Eda H, Mishima Y, Nemani N, Hu Y, Mimura N, Cottini F, Gorgun G et al.. (2013)
Small-molecule multi-targeted kinase inhibitor RGB-286638 triggers P53-dependent and -independent anti-multiple myeloma activity through inhibition of transcriptional CDKs.
Leukemia, 27 (12): 2366-75. [PMID:23807770]
2. van der Biessen DA, Burger H, de Bruijn P, Lamers CH, Naus N, Loferer H, Wiemer EA, Mathijssen RH, de Jonge MJ. (2014)
Phase I Study of RGB-286638, A Novel, Multitargeted Cyclin-Dependent Kinase Inhibitor in Patients with Solid Tumors.
Clin Cancer Res, 20 (18): 4776-83. [PMID:25024258]