NanoBRET® TE Intracellular RAF Dimer Assays Technical Manual
Instructions for Use of Product(s)
N8014, N8015, N8016, N8017
Literature # TM716
The NanoBRET® Target Engagement (TE) Assays measure compound binding at select target proteins within intact cells and have been applied successfully to study multiple target classes. Here we describe a NanoBRET® TE method to measure compounds binding to intracellular dimeric forms of RAF kinases (ARAF, BRAF and CRAF) that are formed in the presence of the constitutively active mutant KRAS(G12C).
RAF kinases play an important role in signaling through the MAPK pathway, one of the most heavily mutated pathways in cancers. RAF dimers are important drug targets for various cancers, especially those driven by mutant RAS proteins. Specifically, the NanoBRET® TE Intracellular RAF Dimer Assays measure compound engagement to the three individual RAF protomers (ARAF, BRAF or CRAF) within RAF heterodimers as well as target engagement at both BRAF and CRAF homodimers.
Summary of Changes
The following changes were made to the 4/24 revision of this document:
1. In Section 4.C, Step 1, Note b. “heterodimer” was changed to “homodimer”.
2. NanoBRET was updated to a registered trademark.
Revised 4/24.