Name: Regorafenib monohydrate
Price: 199.00 USD

- Overview
  - Please contact us at for specific academic pricing.
    
    Background
    
    Regorafenib monohydrate is a multitargetedinhibitor of tyrosine kinase with IC50 values of 13nM, 4.2nM, 46nM, 2.5nM, 28nM, 19nM, 202nM, 22nM, 7nM, 1.5nM and 311nM, respectively for VEGFR-1, mVEGFR-2, mVEGFR-3, Raf-1, BRAF WT, BRAFV600E, FGFR-1, PDGFR-β, c-KIT, RETand TIE2 [1].Regorafenib is a multikinase inhibitor of both intracellular and membrane-bound RTKs. It shows potent inhibition of angiogenic and stromal RTKs like VEGF receptors-1-3, PDGFR-β and FGF receptor-1 with IC50 values ranging from4.2 to 311nM in biochemical assays. It also inhibits oncogenic RTKs, such as RET and c-KIT, with IC50 values ranging from 1.5 to 28nM in cellular assays [1]. Regorafenib is reported to have anti-tumor efficacy to various tumors including breast, pancreas, thyroid, melanoma, GIST, and CRC with a mean IC50 value less than 1μM. These inhibition effects of tumor growth are also found in mouse xenograft models after the treatment of regorafenib at dose ranging from 10 to 100 mg/kg [1].
    
    [1] Crona DJ, Keisler MD, Walko CM.Regorafenib: a novel multitargeted tyrosine kinase inhibitor for colorectal cancer and gastrointestinal stromal tumors.Ann Pharmacother. 2013 Dec;47(12):1685-96.
- Properties
  - Alternative Name
    
    BAY 73-4506 monohydrate; 4-[4-[[4-chloro-3-(trifluoromethyl)phenyl]carbamoylamino]-3-fluorophenoxy]-N-methylpyridine-2-carboxamide;hydrate
    
    CAS Number
    
    1019206-88-2
    
    Molecular Formula
    
    C21H17ClF4N4O4
    
    Molecular Weight
    
    500.83
    
    Appearance
    
    A solid
    
    Purity
    
    98.93%
    
    Solubility
    
    ≥25.05 mg/mL in DMSO; insoluble in H2O
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only

Regorafenib monohydrate

Regorafenib monohydrate

Background

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