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Synonyms: ARO-002 | CP 868596 | CP-868,596 | CP-868596
Compound class: Synthetic organic
Comment: Crenolanib (CP-868,596) is a potent and orally bioavailable benzamidazole Type I inhibitor of wild-type and mutant isoforms of the class III receptor tyrosine kinases FLT3 (FMS-like tyrosine kinase 3), PDGFRα (platelet-derived growth factor receptor), and PDGFRβ [1-3]. It preferentially binds to phosphorylated active kinases in the 'DFG in' conformation.
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. Heinrich MC, Griffith D, McKinley A, Patterson J, Presnell A, Ramachandran A, Debiec-Rychter M. (2012)
Crenolanib inhibits the drug-resistant PDGFRA D842V mutation associated with imatinib-resistant gastrointestinal stromal tumors.
Clin Cancer Res, 18 (16): 4375-84. [PMID:22745105]
2. Smith CC, Lasater EA, Lin KC, Wang Q, McCreery MQ, Stewart WK, Damon LE, Perl AE, Jeschke GR, Sugita M et al.. (2014)
Crenolanib is a selective type I pan-FLT3 inhibitor.
Proc Natl Acad Sci USA, 111 (14): 5319-24. [PMID:24623852]
3. Zimmerman EI, Turner DC, Buaboonnam J, Hu S, Orwick S, Roberts MS, Janke LJ, Ramachandran A, Stewart CF, Inaba H et al.. (2013)
Crenolanib is active against models of drug-resistant FLT3-ITD-positive acute myeloid leukemia.
Blood, 122 (22): 3607-15. [PMID:24046014]