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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).
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.
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.
Storage Stability: Up to 6 months when stored as recommended.
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.
Warnings: Avoid freeze/thaw cycles.
Biosafety Level: Not applicable (BSL-1)
References: 1. Ostrem, J. M., et al., Nature. 2013; 503:548-551.
2. Patricelli, M. P., et al., Cancer Discovery. 2016; 6:316-329
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