KRAS(G12C) Nucleotide Exchange Assay Kit

DESCRIPTION

The KRAS(G12C) Nucleotide Exchange Assay Kit is designed for screening and profiling of KRAS(G12C) antagonists/inhibitors by using BODIPY-GDP to monitor the GDP or GTP binding status. The kit can be used with two different protocols for greater flexibility, either titrating the inhibitor with fixed GTP concentration or titrating the GTP with fixed inhibitor concentration.

DETAILS

Shiptemp: -80°C (dry ice)
Synonyms: C-K-RAS kit, CFC2 kit, K-RAS2A kit, Nucleotide Exchange Assay
Warnings: Avoid freeze/thaw cycles.
Category: Cell Based Assay Kit/Cell Signaling Pathway
Background: It is well established that RAS mutations are responsible more than 30% of human cancers and KRAS(G12C) is one of the KRAS mutations that is found frequently in lung and colon cancers. Recent studies discovered a small molecule called AMG510 (Amgen) that can block the KRAS(G12C)-mediated signaling pathway by locking the KRAS conformation in the GDP-bound state. Compounds that affect the nucleotide exchange (GDP to GTP) reaction in KRAS could lead to a novel approach to the inhibition of tumor cell growth in KRAS(G12C)-driven tumors.
References: 1. Ostrem, J. M., et al., Nature. 2013; 503:548-551. 2. Patricelli, M. P., et al., Cancer Discovery. 2016; 6:316-329
Description: The KRAS(G12C) Nucleotide Exchange Assay Kit is designed for screening and profiling of KRAS(G12C) antagonists/inhibitors by using BODIPY-GDP to monitor the GDP or GTP binding status. The kit can be used with two different protocols for greater flexibility, either titrating the inhibitor with fixed GTP concentration or titrating the GTP with fixed inhibitor concentration.
Methodology: Fluorescence Polarization
Supplied As: The KRAS(G12C) Nucleotide Exchange Assay Kit comes in a convenient 384-well format, with enough purified recombinant KRAS(G12C) labeled with BODIPY-GDP, GTP, and assay buffer and additives for 400 enzyme reactions.
Unspsc Code: 41105332
Unspsc Name: Protein chemiluminescent detection reagents or kits or substrates
Applications: Useful for screening small molecular inhibitors/antagonists that are expected to affect the KRAS(G12C)-GDP or -GTP binding status for drug discovery and HTS targeting of KRAS(G12C).
Product Type: Assay Kit
Biosafety Level: Not applicable (BSL-1)
Related Products: 100413, 100479, 100480, 11308
Storage Stability: Up to 6 months when stored as recommended.
Scientific Category: Cell Signaling Pathway
Instructions for Use: See assay kit datasheet for detailed protocol.