XMD8-87 is an inhibitor of tyrosine kinase non-receptor 2 (TNK2) with an IC50 value of 1.9 μM in HEK293T cells expressing human TNK2. It is selective for TNK2 over a panel of approximately 100 kinases with >90 and <50% inhibition for TNK2 and all other kinases tested, respectively. XMD8-87 inhibits growth of Ba/F3 cells expressing constitutively active mutant TNK2s (IC50s = 0.1-77 nM) commonly found in leukemias but has no effect on cells expressing wild-type TNK2 (IC50 = >1 μM).
