| Description: |
XMD8-87 is a potent TNK2 inhibitor with IC50 values of 38 and 113 nM for the D163E and R806Q mutations, respectively. |
| Target: |
IC50: 38 nM (TNK2, D163E mutation), 113 nM (TNK2, R806Q mutation)[1] |
| In Vitro: |
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] |
| Kinase Assay: |
Kinase targets are tested with biochemical enzymatic kinase assays using the SelectScreen Kinase Profiling Service to determine IC50 values. The compounds (XMD8-87) are assayed at 10 concentrations (3-fold serial dilutions starting from 1 μM) at an ATP concentration equal to the ATP Km[1]. |
| Cell Assay: |
Cells are treated with the following inhibitors for 72 hours: dasatinib, AIM-100, XMD8-87 and XMD16-5. Cell viability is measured using a methanethiosulfonate (MTS)-based assay and absorbance (490 nm) is read at 1 and 3 hours after adding reagent[1]. |
| Animal Administration: |
[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. |
