Pexmetinib (ARRY-614) is a potent, orally active, dual Tie-2/p38 MAPK inhibitor with IC50 of 1, 26 and 35 nM for Tie-2, p38α and p38β, respectively.
Pexmetinib (ARRY-614) demonstrates in vitro mechanistic models (Angpt-1 or anisomycin-stimulated HUVEC) as well as functional readouts (LPS-induced TNF-alpha release from human PBMCs) with IC50 of 2282 nM and 172 nM for Tie2 and p38, respectively.
Pexmetinib (ARRY-614) abrogates cytokine mediated myelosuppresive effects in hematopoietic cells.
Pexmetinib (ARRY-614) inhibits leukemic cell proliferation and stimulates hematopoietic activity in MDS.
Pexmetinib (ARRY-614) inhibits LPS-induced TNF-alpha release) murine models .
