-
-
Overview
-
Please contact us at for specific academic pricing.
Background
GS-9973 is a selective inhibitor of Syk with IC50 value of 7.7 nM [1].
Spleen tyrosine kinase (Syk) is a cytoplasmic tyrosine kinase that is expressed mainly in hematopoietic cells and acts as a mediator of immunoreceptor signaling. Syk can be used for therapy of autoimmune, oncology indications and allergy [1].
GS-9973 is an orally bioavailable and selective Syk inhibitor. GS-9973 showed good absorption potential and high bioavailability. In monocytes, GS-9973 inhibited immune-complex-stimulated cytokine production and BCR-mediated proliferation and activation of B-cells [1]. In chronic lymphocytic leukemia (CLL) cells, GS-9973 significantly reduced pAkt and ribosomal S6 phosphorylation. These results suggested that GS-9973 inhibited B-cell receptor (BCR) mediated signaling pathways. In CLL samples, the combination of GS-9973 and idelalisib synergistically reduced CLL cell viability [2].
In chronic lymphocytic leukemia patients, GS-9973 inhibited adenopathy and reduced lymph node [3].[1]. Currie KS, Kropf JE, Lee T, et al. Discovery of GS-9973, a selective and orally efficacious inhibitor of spleen tyrosine kinase. J Med Chem, 2014, 57(9): 3856-3873.
[2]. Burke RT1, Meadows S, Loriaux MM, et al. A potential therapeutic strategy for chronic lymphocytic leukemia by combining Idelalisib and GS-9973, a novel spleen tyrosine kinase (Syk) inhibitor. Oncotarget, 2014, 5(4): 908-915.
[3]. Sharman J, Hawkins M, Kolibaba K, et al. An open-label phase 2 trial of entospletinib (GS-9973), a selective spleen tyrosine kinase inhibitor, in chronic lymphocytic leukemia. Blood, 2015, 125(15): 2336-2343.
-
- Properties
-
Overview
- Home
- Products
- Life Science
- Analytical Chromatography
- Assay Kits
- Biochemical Reagents
- Antibodies
- Antigens
- Enzymes
- Chemicals
- Proteins
- Liposomes
- Cell Culture
- Cell Analysis
- Cloning and Expression
- Nucleic Acid Synthesis
- Nucleic Acid Extraction
- Nucleic Acid Electrophoresis
- PCR
- Protein Gel Electrophoresis
- Protein Biochemistry
- Nanoparticles
- Glycan Analysis
- Immunohistochemistry (IHC)
- Microbiology
- Biospecimens
- Transfection Reagents
- Ion Exchange Resins
- Venoms
- Lab Solutions
- Lab Equipment
- Biosensors
- Flow Imaging Microscopes
- Fluorescence Quality Management Solutions
- Electrophoresis Systems
- Hematology Analyzers
- Isothermal Amplification Instruments
- Liquid Handling Equipment
- Luminometers
- Microfluidic Flow Control Systems
- Next-generation Sequencing Systems
- Nucleic Acid Purification Instruments
- Raman Spectroscopy Systems
- Sample Tracking Systems
- Spectrometer Accessories
- Syringe Pumps
- Thawing and Warming Systems
- Tissue Dissociation Systems
- Water Purification Systems
- Western Blotting Equipment
- General Laboratory Equipment
- Clinical Chemistry Analyzers
- Amerigo Scientific Instrument
- Automated Cell Selection Systems
- Automated Nucleic Acid Extraction Instruments
- Balances, Scales and Weighing
- Biolayer Interferometry Instruments
- Bioprocess Filtration Equipment
- Bioprocess Systems and Accessories
- Bioreactors and Fermenters
- Cappers and Decappers
- Cell Thawing Instruments
- Chromatography
- Data Loggers
- Droplet Generators
- Dry Baths
- Flow Cytometers
- Histology Laboratory Equipment
- Lab Ovens and Furnaces
- Lab Refrigeration Equipment
- Lab Shakers and Mixers
- Laboratory Centrifuges
- Laboratory Evaporators
- Laboratory Hoods
- Laboratory Incubators
- Laboratory Microscopes
- Laboratory Mills
- Laboratory Pumps
- Liquid Handling
- Live Cell Imaging Systems
- Microbiology Equipment
- Microscopy Flow Cells
- Mutation Breeding Instruments
- Oligonucleotide Synthesis Devices
- Particle Counters
- Plasma Surface Treatment Equipment
- Presses and Pellet Dies
- Surface Plasmon Resonance Instruments
- Ultrasonic Cleaners
- UV Disinfection Systems
- VOC Analysis Equipment
- VPHP Sterilization Systems
- Water Baths
- Lab Equipment
- Diagnostics & Clinical
- Applied Science
- Life Science
- Services
- About Us
- Contact Us
.
