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

Description

raw data for avapritinib derivatives (NMR spectra and mass spec); cell titer glo results testing midostaurin and avapritinib against varied KIT gatekeeper mutations in Ba/F3 cells and 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