Products from BPS Bioscience require a minimum order value above 400€
Application: Screen small molecule inhibitors or antagonists that affect KRAS(G12C) nucleotide-binding status in high throughput screening (HTS) applications.
Background: It is well established that RAS mutations are responsible for more than 30% of human cancers. KRAS(G12C) is one of the KRAS mutations that is found frequently in lung and colon carcinomas. The G12C mutation favors the activated (GTP-bound) state of KRAS, amplifying signaling pathways that lead to oncogenesis. Recent studies have led to the discovery of a small molecule called AMG510 (Amgen) that locks KRAS conformation in the GDP-bound (inactive) state, thereby blocking KRAS(G12C)-mediated signaling pathway. Compounds that affect the nucleotide exchange (GDP to GTP) reaction could lead to a novel approach leading to the inhibition of tumor cell growth in KRAS(G12C) driven tumors.
Contraindications: This kit is compatible with up to 1% final DMSO concentration. Compounds that are fluorescent may interfere with the results, depending on their spectral excitation and emission properties.It is recommended that the compound alone is tested to determine any potential interference of the compound on the assay results.
Description: The KRAS (G12C) Isoform A Coupled Nucleotide Exchange TR-FRET Assay Kit is a TR-FRET (Time-Resolved Fluorescence Resonance Energy Transfer) assay kit designed for screening and profiling of KRAS (Kirsten rat sarcoma) (G12C) antagonists/inhibitors. It monitors the binding of an effector protein such as the Ras binding domain of Raf1, (RBD-cRAF), to KRAS(G12C). The KRAS(G12C) Isoform A Coupled Nucleotide Exchange TR-FRET Assay Kit comes in a convenient 384-well format, with enough purified recombinant GDP-loaded KRAS(G12C) Isoform A, GTP, exchange factor SOS1 (son of sevenless homolog 1) (amino acids 564-1049), effector protein RBD-cRAF (amino acids 50-140), assay buffer and additives for 400 reactions.
Storage Stability: This assay kit will perform optimally for up to 6 months from date of receipt when the materials are stored as directed.
Uniprot: P01116
Warnings: Avoid freeze/thaw cycles
Biosafety Level: Not applicable (BSL-1)
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