Description
A multi-kinase inhibitor; inhibits Lck, VEGFR2/KDR, p38α, and JAK3 (IC50s = 0.2, 1, 3, and 72 nM, respectively); selective for these kinases over a panel of additional kinases including SYK, JNK1, and PKAβ (IC50s = 292 to >25,000 nM) but does inhibit Src (IC50 = 2 nM); inhibits T cell proliferation in vitro in a mixed lymphocyte reaction assay (IC50 = 30 nM); decreases production of IL-2 induced by an anti-CD3 antibody in mice at 10, 30, and 100 mg/kg; decreases levels of mutant oncogene KRASG12V in HeLa cells in a reporter assay at 1 µM