KRAS (G12V) NanoBRET Target Engagement Intracellular Ras Assay for screening of compounds binding to the target.
KRAS2B, KRAS2A, KRAS4A, KRAS4B, RASK2
HEK293 human epithelial cell line from ATCC
384-well plate format using Promega’s NanoBRET TE Intracellular Ras Assay
HEK293 cells transiently expressing LgBiT®-KRAS (G12V) and SmBiT®-KRAS (G12V) Fusion Vectors were seeded into the wells of 384-well plates. The cells were pre-treated with the NanoBRET Tracer K-1 and then treated with reference compound BI-2852 for 2 hours. The BRET signal was measured on an Envision 2104 Multilabel Reader. IC50 value was calculated and IC50 curve was plotted using the GraphPad Prism 4 program based on a sigmoidal dose response equation.
Binding of compound to target Ras