Name: JNJ-38877605
Price: 254.00 USD

- Overview
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    Background
    
    JNJ-38877605 is a small-molecule ATP-competitive inhibitor of the catalytic activity of c-Met.
    Extensive evidence that c-Met signaling is involved in the progression and spread of several cancers and an enhanced understanding of its role in disease have generated considerable interest in c-Met and HGF asmajor targets in anti-cancer drug development.
    In vitro: JNJ-38877605 showed ~600-fold selectivity for c-Met compared with a panel of ~250 diverse tyrosine and serine-threonine kinases and was found to potently inhibit HGF-stimulated and constitutively activated c-Met phosphorylation in vitro [1].
    In vivo: JNJ-38877605 showed excellent oral bioavailability approaching 100% in all examined species. In addition, JNJ-38877605 in a single dose was observed toinhibit Met phosphorylation in tumor xenografts for up to16 h. Inhibition of Met phosphorylation was associated withdose-dependent tumor growth inhibition using a range of oral dosing regimens [2].
    Clinical trial: A Safety and Dose-finding Study of JNJ-38877605 in Patients With Advanced or Refractory Solid Tumors.
    
    [1] PereraT, L avrijssenT, Janssens B, et al. JNJ-38877605: a selective Met kinase inhibitor inducingregression of Met-driven tumor models. Presented at the 99th AACR Annual Meeting; 2008 Apr 12 -16;
- Properties
  - Alternative Name
    
    6-[difluoro-[6-(1-methylpyrazol-4-yl)-[1,2,4]triazolo[4,3-b]pyridazin-3-yl]methyl]quinoline
    
    CAS Number
    
    943540-75-8
    
    Molecular Formula
    
    C19H13F2N7
    
    Molecular Weight
    
    377.35
    
    Purity
    
    98.00%
    
    Solubility
    
    insoluble in H2O; ≥18.85 mg/mL in DMSO; ≥3.25 mg/mL in EtOH with ultrasonic
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only

JNJ-38877605

JNJ-38877605

Background

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