KRAS (G12D)/cRAF NanoBRET RAS Assay

KRAS (G12D)/cRAF NanoBRET Target Engagement Intracellular RAS Assay for screening of compounds binding to the target.

Target Overview

Target

KRAS (G12D)/cRAF

HGNC Symbol

KRAS, RAF1

Synonyms

KRAS4B, RAF1

Cell Line

HEK293 human epithelial cell line from ATCC

Assay Properties

Assay Format

384-well plate format using the NanoBRET Intracellular KRAS (G12D)/cRAF Interaction Assay

Assay Protocol

HEK293 cells transiently expressing Nanoluc-KRAS G12D_cRAF FL Halotag BiBRET Vector were seeded into the wells of 384-well plates. The cells were pre-treated with HaloTag NanoBRET 618 Ligand and then treated with reference compound RMC-6236 (Daraxonrasib) for 24 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 program based on a sigmoidal dose response equation.

Readout

Blockade of Cellular KRAS (G12D)/cRAF Interaction by compound

Reference Compound IC50s

Compounds	IC50 (M)
RMC-6236 (Daraxonrasib)	9.944e-009

Screening Location

Malvern, PA, USA

Further Information

More information can be found on our website RAS Assays for Drug Discovery.

Reference Compound IC50 for KRAS (G12D)/cRAF Interaction

Reference Compound IC50 for KRAS (G12D)/cRAF interaction

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