- Advanced search
- Immuno Portal
- Malaria Portal
Synonyms: PLX-3397 | PLX3397 | Turalio®
pexidartinib is an approved drug (FDA (2019))
Compound class: Synthetic organic
Comment: Pexidartinib is an orally available, multi-targeted inhibitor of the receptor tyrosine kinases, Fms-related tyrosine kinase 3 (FLT3), stem cell growth factor receptor (KIT) and colony stimulating factor 1 receptor (CSF1R), with potential antineoplastic activity . Pexidartinib is compound P-0181 in patent US7893075 B2 .
It is active against wild type FLT3 and the FLT3 gatekeeper F691L resistance mutant, but its activity is vulnerable to mutations in the FLT3 activation loop .
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. Cupp JS, Miller MA, Montgomery KD, Nielsen TO, O'Connell JX, Huntsman D, van de Rijn M, Gilks CB, West RB. (2007)
Translocation and expression of CSF1 in pigmented villonodular synovitis, tenosynovial giant cell tumor, rheumatoid arthritis and other reactive synovitides.
Am J Surg Pathol, 31 (6): 970-6. [PMID:17527089]
2. Fiocco U, Sfriso P, Lunardi F, Pagnin E, Oliviero F, Scagliori E, Cozzi L, Vezzù M, Molena B, Scanu A et al.. (2010)
Molecular pathways involved in synovial cell inflammation and tumoral proliferation in diffuse pigmented villonodular synovitis.
Autoimmun Rev, 9 (11): 780-4. [PMID:20620241]
3. Molena B, Sfriso P, Oliviero F, Pagnin E, Teramo A, Lunardi F, Stramare R, Scanu A, Nardacchione R, Rubaltelli L et al.. (2011)
Synovial colony-stimulating factor-1 mRNA expression in diffuse pigmented villonodular synovitis.
Clin Exp Rheumatol, 29 (3): 547-50. [PMID:21640049]
4. Smith CC, Zhang C, Lin KC, Lasater EA, Zhang Y, Massi E, Damon LE, Pendleton M, Bashir A, Sebra R et al.. (2015)
Characterizing and Overriding the Structural Mechanism of the Quizartinib-Resistant FLT3 "Gatekeeper" F691L Mutation with PLX3397.
Cancer Discov, 5 (6): 668-79. [PMID:25847190]
5. Tap WD, Wainberg ZA, Anthony SP, Ibrahim PN, Zhang C, Healey JH, Chmielowski B, Staddon AP, Cohn AL, Shapiro GI et al.. (2015)
Structure-Guided Blockade of CSF1R Kinase in Tenosynovial Giant-Cell Tumor.
N Engl J Med, 373 (5): 428-37. [PMID:26222558]
6. Zhang J, Ibrahim PN, Artis DR, Bremer R, Wu G, Zhu H, Nespi M, Zhang C. (2011)
Compounds modulating c-fms and/or c-kit activity and uses therefor.
Patent number: US7893075 B2. Assignee: Plexxikon, Inc.. Priority date: 22/11/2006. Publication date: 22/02/2011.