Name: Golvatinib (E7050)
Price: 286.00 USD

- Overview
  - Please contact us at for specific academic pricing.
    
    Background
    
    Golvatinib is an inhibitor of c-Met and VEGFR-2 tyrosine kinase with IC50 values of 14nM and 16nM, respectively [1].The small molecule compound, golvatinib, is a dual inhibitor of both c-Met and VEGFR-2. It is developed as a therapeutic reagent with more potent antitumor activity. Golvatinib inhibits the autophosphorylation of c-Met in MKN45 cells and inhibits the phosphorylation of VEGFR-2 in HUVECs with IC50 values of 14nM and 16nM, respectively. Golvatinib also inhibits the growth of various tumor cells including MKN45, EBC-1, Hs746T and SNU-5. Besides that, golvatinib effectively suppresses the growth induced by HGF or VEGF with IC50 values of 17nM and 84nM [1]. In mice models bearing xenograft tumor cell lines including MKN45, Hs746T, SNU-5 and EBC-1, treatment of golvatinib significantly inhibits the tumor growth. In mice xenograft model with VEGF-overexpressed human pancreatic cancer cell line KP-1 /VEGF, a single administration of E7050 reduces the VEGFR-2 phosphorylation and subsequently inhibits tumor growth through inhibiting VEGF /VEGFR-2 mediated tumor angiogenesis [1].
    
    [1] Nakagawa T, Tohyama O, Yamaguchi A, et al. E7050: A dual c-Met and VEGFR-2 tyrosine kinase inhibitor promotes tumor regression and prolongs survival in mouse xenograft models. Cancer science, 2010, 101(1): 210-215.
- Properties
  - Alternative Name
    
    1-N'-[2-fluoro-4-[2-[[4-(4-methylpiperazin-1-yl)piperidine-1-carbonyl]amino]pyridin-4-yl]oxyphenyl]-1-N-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide
    
    CAS Number
    
    928037-13-2
    
    Molecular Formula
    
    C33H37F2N7O4
    
    Molecular Weight
    
    633.69
    
    Appearance
    
    A solid
    
    Purity
    
    98.00%
    
    Solubility
    
    insoluble in H2O; ≥1.39 mg/mL in EtOH with ultrasonic; ≥15.85 mg/mL in DMSO with gentle warming
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only

Golvatinib (E7050)

Golvatinib (E7050)

Background

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