-
-
Overview
-
Please contact us at for specific academic pricing.
Background
Crenolanib (CP-868596) is a potent, specific, and orally available inhibitor of PDGFRα, PDGFRβ and FLT3 with inhibitor-binding constant (Kd) of 3.2, 2.1, and 0.74 nM, respectively [1].
It has been shown that crenolanib is more potent than quizartinib and sorafenib at blocking FLT3 autophosphorylation and causing cytotoxicity [2]. Crenolanib is confirmed to be100-fold more potent than imatinib at suppressing D842V mutation. In addition, it has been reported that crenolanib inhibits PDGFRα D842V mutation rather than V561D mutation, with IC50 value of 10 nM [1]. In EOL-1 cells, crenolanib also inhibits the FIP1L1-PDGFRA fusion kinase activity (IC50=1 nM) and cell proliferation (IC50= 0.2 pM)[1].[1] Heinrich MC1, Griffith D, McKinley A, Patterson J, Presnell A, Ramachandran A, Debiec-Rychter M.
Crenolanib inhibits the drug-resistant PDGFRA D842V mutation associated with imatinib-resistant gastrointestinal stromal tumors. Clin Cancer Res. 2012 Aug 15;18(16):4375-84.
[2] Galanis A1, Ma H, Rajkhowa T, Ramachandran A, Small D, Cortes J, Levis M. Crenolanib is a potent inhibitor of FLT3 with activity against resistance-conferring point mutants. Blood. 2014 Jan 2;123(1):94-100.
-
- Properties
- Reference
-
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
.
