KRAS (G12C) NanoBRET RAS Assay

KRAS (G12C) NanoBRET Target Engagement Intracellular RAS Assay for screening of compounds binding to the target.

Target Overview

Target

KRAS (G12C)

HGNC Symbol

KRAS

Synonyms

KRAS2B, KRAS2A, KRAS4A, KRAS4B, RASK2

Cell Line

HEK293 human epithelial cell line from ATCC

Assay Properties

Assay Format

384-well plate format using Promega’s NanoBRET TE Intracellular RAS Assay

Assay Protocol

HEK293 cells transiently expressing LgBiT®-KRAS(G12C) and SmBiT®-KRAS(G12C) Fusion Vectors were seeded into the wells of 384-well plates. The cells were pre-treated with the NanoBRET RAS Tracer K-1 and then treated with reference compounds ARS1620 and AMG510 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 program based on a sigmoidal dose response equation.

Readout

Binding of compound to target RAS

Reference Compound IC50s

Compounds	IC50 (M)
ARS1620	1.203e-008
AMG510	9.989e-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 (G12C)

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