1234480-46-6

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).

XMD8-87 is used in the studies of benzopyrimidodiazepinones as most selective and potent ERK5 inhibitor.

[1] MAXSON J E, ABEL M L, WANG J, et al. Data from Identification and Characterization of Tyrosine Kinase Nonreceptor 2 Mutations in Leukemia through Integration of Kinase Inhibitor Screening and Genomic Analysis[C]//1 1. 2023: 0. DOI: 10.1158/0008-5472.c.6507081