XMD8-87 is a potent TNK2 inhibitor with IC50 values of 38 and 113 nM for the D163E and R806Q mutations, respectively.
XMD8-87 potently inhibits the growth of the TNK2 mutant expressing cell lines while having little or no effect on the control cells out to the highest tested concentrations (1,000 nM). XMD8-87 has IC50s of 38 nM and 113 nM for the D163E and R806Q mutations. The effects of XMD8-87 on TNK2 cell lines are largely due to on-target effects on TNK2. Auto-phosphorylation of overexpressed TNK2 mutants could be blocked with TNK2 inhibitor XMD8-87[1].
References:
[1]. Maxson JE, et al. Identification and Characterization of Tyrosine Kinase Nonreceptor 2 Mutations in Leukemia through Integration of Kinase Inhibitor Screening and Genomic Analysis.