TAK-659 hydrochloride (Mivavotinib, TAK659) is a potent, selective and orally available SYK inhibitor with IC50 of 3.2 nM.
TAK-659 displays 36, 42 and 23-fold selectivity over JAK3, ZAP70 and VEGFR2, respectively.
TAK-659 also potently inhibits FLT-3; inhibits cellular proliferation in SYK-dependent DLBCL and FLT3-dependent AML cell lines, demonstrates potent tumor growth inhibition in the FLT3-dependent MV4-11 xenograft models.
