JNJ-10198409

- Overview
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    Background
    
    JNJ-10198409 is a small molecule inhibitor of platelet-derived growth factor (PDGF-BB) tyrosine kinase [1].Platelet-derived growth factor (PDGF) is a ubiquitous mitogen involved in regulating cell growth and division, embryonic development, cell proliferation, cell migration, and angiogenesis. Overexpression of PDGF has been associated with several diseases such as atherosclerosis, fibrotic disorders and malignancies. Inhibition of the tyrosine kinase activity of growth factor receptors such as the platelet-derived growth factor (PDGF-BB) receptor can have potent antiangiogenic and antiproliferative activity. Recombinant PDGF is used in medicine to help heal chronic ulcers and in orthopedic surgery and periodontistry to treat bone loss [2].In human coronary artery smooth muscle cells, JNJ-10198409 inhibited the activity of platelet-derived growth factor (PDGF-BB) tyrosine kinase with an IC50 value of 4.2 nM when tested. JNJ-10198409 was a competitive antagonist of the ATP binding and hydrolysis at PDGF-BB receptor, resulting in a dose dependent inhibition of tumor growth and angiogenesis [1].
    
    [1] Ho C Y, Ludovici D W, Maharoof U S M, et al. (6, 7-Dimethoxy-2, 4-dihydroindeno [1, 2-c] pyrazol-3-yl) phenylamines: Platelet-derived growth factor receptor tyrosine kinase inhibitors with broad antiproliferative activity against tumor cells[J]. Journal of medicinal chemistry, 2005, 48(26): 8163-8173.
    [2] Raines E W, Bowen-Pope D F, Ross R. Platelet-derived growth factor[M]//Peptide growth factors and their receptors I. Springer Berlin Heidelberg, 1990: 173-262.
- Properties
  - Alternative Name
    
    (Z)-N-(6,7-dimethoxy-1,2-dihydroindeno[1,2-c]pyrazol-3(4H)-ylidene)-3-fluoroaniline
    
    CAS Number
    
    627518-40-5
    
    Molecular Formula
    
    C18H16FN3O2
    
    Molecular Weight
    
    325.34
    
    Appearance
    
    A crystalline solid
    
    Purity
    
    98.00%
    
    Solubility
    
    ≤10mg/ml in ethanol;30mg/ml in DMSO;30mg/ml in dimethyl formamide
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only

JNJ-10198409

Background

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