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Synonyms: ARRY-614 | ARRY614
Compound class: Synthetic organic
Comment: Pexmetinib is an orally bioavailable small-molecule inhibitor of p38 MAPK (β isoforms) and Tie2 kinases . It is a type 2 kinase inhibitor that binds both Tie2 and p38 MAP kinases in the "DFG-out" conformation. p38 MAPK is a proinflammatory kinase, Tie2 is an endothelial cell specific receptor tyrosine kinase and is the receptor for angiopoietin-1. Concomitant inhibition of these kinases is predicted to produce antineoplastic, anti-inflammatory and antiangiogenic effects that would provide a novel anti-cancer therapeutic, in particular for the treatment of myelodysplastic syndromes (MDS) [1,4] and acute myeloid leukemia (AML).
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. Bachegowda L, Gligich O, Mantzaris I, Schinke C, Wyville D, Carrillo T, Braunschweig I, Steidl U, Verma A. (2013)
Signal transduction inhibitors in treatment of myelodysplastic syndromes.
J Hematol Oncol, 6: 50. [PMID:23841999]
2. Bachegowda L, Morrone K, Winski SL, Mantzaris I, Bartenstein M, Ramachandra N, Giricz O, Sukrithan V, Nwankwo G, Shahnaz S et al.. (2016)
Pexmetinib: A Novel Dual Inhibitor of Tie2 and p38 MAPK with Efficacy in Preclinical Models of Myelodysplastic Syndromes and Acute Myeloid Leukemia.
Cancer Res, 76 (16): 4841-4849. [PMID:27287719]
3. Garcia-Manero G, Khoury HJ, Jabbour E, Lancet J, Winski SL, Cable L, Rush S, Maloney L, Hogeland G, Ptaszynski M et al.. (2015)
A phase I study of oral ARRY-614, a p38 MAPK/Tie2 dual inhibitor, in patients with low or intermediate-1 risk myelodysplastic syndromes.
Clin Cancer Res, 21 (5): 985-94. [PMID:25480830]
4. Gañán-Gómez I, Bohannan ZS, Garcia-Manero G. (2015)
p38 MAPK in MDS.
Aging (Albany NY), 7 (6): 346-7. [PMID:26081220]