KIT gatekeeper mutations cause avapritinib resistance via dynamical changes in the kinase domain

Description

raw data for avapritinib derivatives (NMR spectra) and cell titer glo results testing avapritnib derivatives against Ba/F3 KIT D816V and Ba/F3 D816V + T670I cells

Steps to reproduce

For the cell titer glo assays: Ba/F3 cells expressing either KIT D816V or KIT D816V+T670I were plated at 2000 cells per well in 96-well white opaque tissue culture plates (Corning) and treated with inhibitor at 10-fold dilutions (concentrations are shown on data sheets) or DMSO. After 48 hours, cell proliferation was assessed with the CellTiter-GLO luminescent cell viability assay (Promega). IC50s were then calculated with GraphPad Prism 10. For the compound characterization: all methods are included in the document provided.

Institutions

• University of California San Francisco

  CA, San Francisco

Categories

Funders

• Bachrach Family Foundation

Licence