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Application: Study enzyme kinetics and screen small molecule inhibitors for drug discovery and high throughput screening (HTS) applications.
Background: ROS1 (proto-oncogene ROS1), also known as c-ROS, is a type I tyrosine kinase receptor of the insulin receptor family. This protein is involved in cell differentiation and proliferation. ROS1 can act with multiple adaptor proteins involved in PI3K (phosphoinositide 3-kinase)/AKT, JAK (Janus kinase)/STAT3 (signal transducer and activator of transcription 3) and other signaling pathways. Mutations, rearrangements, and fusions of this gene can promote proliferation of tumor cells, such as in NSCLC (non-small cell lung cancer), with gene fusions being the highest driving force in tumor development and progression. For instance, fusion to CD74 is found in 38% of the ROS1+ NSCLCs. The specific gene fusions localize the protein in different cellular compartments and thus leads to activation of different pathways. Overexpression was found in primary gliomas and meningiomas. The use of crizotinib and ceritinib, two ROS1-targeting TKIs (tyrosine kinase inhibitors), has been approved for use in ROS1+ NSCLC. However, there are concerns with the development of drug resistance, due to mutation or activation of alternative signaling pathways, and side effects that range from edema to neutropenia, as ROS1 inhibitors are multi-kinase inhibitors. Next-generation inhibitors with higher affinity are currently in clinical trials and promise improved outcomes in the treatment of ROS1-related disorders.
Contraindications: The final concentration of DMSO in the assay should not exceed 1%.
Description: The Chemi-Verse™ ROS1 Kinase Assay Kit is designed to measure ROS1 (ROS Proto-Oncogene 1) tyrosine kinase activity for screening and profiling applications using ADP-Glo™ as a detection reagent. The assay kit comes in a convenient 96-well format, with enough purified ROS1 kinase domain (amino acids 1883-2347(end)), kinase substrate, ATP, and kinase assay buffer for 100 enzyme 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: P08922
Warnings: Avoid freeze/thaw cycles
Biosafety Level: Not applicable (BSL-1)
References: Li S., et al., 2024 Cancer Med 13(8):e7201.
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