Regorafenib (BAY 73-4506)Catalog No. A10250

Quick Overview

Regorafenib (BAY 73-4506) is a multikinase inhibitor with IC50 of 17, 40 and 69 nM c-KIT, VEGFR2, B-Raf. Regorafenib (BAY 73-4506) is an orally bioavailable multikinase inhibitor targeting both the tumor and its vasculature.
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Regorafenib (BAY 73-4506)

Regorafenib (BAY 73-4506)  Citations(2)
  • Takeshi Uenaka, .et al. In silico drug screening by using genome-wide association study data repurposed dabrafenib, an anti-melanoma drug, for Parkinson-s disease, Hum Mol Genet, 2018, Nov 15; 27(22): 3974-3985 PMID: 30137437
  • Yi Xu, .et al. Knockdown of delta-5-desaturase promotes the anti-cancer activity of dihomo-γ-linolenic acid and enhances the efficacy of chemotherapy in colon cancer cells expressing COX-2, Free Radic Biol Med, 2016, Jul; 96: 67-77 PMID: 27101738
  • Product Information
    Catalog Num A10250
    M. Wt 482.8
    Formula C21H15ClF4N4O3
    Solubility DMSO
    Purity >98%
    Storage at -20°C 3 years Powder
    CAS No. 755037-03-7
    Synonyms N/A
    SMILES Code CNC(=O)C1=NC=CC(=C1)OC2=CC(=C(C=C2)NC(=O)NC3=CC(=C(C=C3)Cl)C(F)(F)F)F

    Biological activity
    Introduction
    Regorafenib (BAY 73-4506) is a multikinase inhibitor with IC50 of 17, 40 and 69 nM c-KIT, VEGFR2, B-Raf. Regorafenib (BAY 73-4506) is an orally bioavailable multikinase inhibitor targeting both the tumor and its vasculature.
    Targets
    Target Value
    RETIC50: 1.5nM
    Raf-1IC50: 2.5nM
    VEGFR2IC50: 4.2nM
    KitIC50: 7nM
    VEGFR1IC50: 13nM
    B-Raf(V600E)IC50: 19nM
    PDGFRβIC50: 22nM
    B-RafIC50: 28nM
    VEGFR3IC50: 46nM
    FGFR1IC50: 202nM
    Tie-2IC50: 311nM
    Solubility
    Solubility (25C) * In vitro DMSO 97 mg/mL (200.9 mM)
    Water <1 mg/mL (<1 mM)
    Ethanol <1 mg/mL (<1 mM)
    In vivo 30% PEG400/0.5% Tween80/5% propylene glycol 30 mg/mL
    * <1 mg/ml means slightly soluble or insoluble.
    * Please note that Adooq tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

    Biological Activity

    Regorafenib (also known as BAY 73-4506) is an oral multi-kinase inhibitor developed by Bayer which targets angiogenic, stromal and oncogenic receptor tyrosine kinase (RTK). Regorafenib shows anti-angiogenic activity due to its dual targeted VEGFR2-TIE2 tyrosine kinase inhibition. It is currently being studied as a potential treatment option in multiple tumor types.

     Regorafenib (BAY 73-4506), a novel oral multikinase inhibitor, potently inhibits these endothelial cell kinases in biochemical and cellular kinase phosphorylation assays. Furthermore, regorafenib inhibits additional angiogenic kinases (VEGFR1/3, platelet-derived growth factor receptor-β, and fibroblast growth factor receptor 1) and the mutant oncogenic kinases c-KIT, RET, and B-RAF. The antiangiogenic effect of regorafenib was demonstrated in vivo by dynamic contrast-enhanced magnetic resonance imaging. Regorafenib administered once orally at 10 mg/kg significantly decreased the extravasation of Gadomer in the vasculature of rat GS9L glioblastoma tumor xenografts. In a daily (qd)×4 dosing study, the pharmacodynamic effects persisted for 48 hr after the last dosing and correlated with tumor growth inhibition (TGI). A significant reduction in tumor microvessel area was observed in a human colorectal xenograft after qd×5 dosing at 10 and 30 mg/kg. Regorafenib exhibited potent dose-dependent TGI in various preclinical human xenograft models in mice, with tumor shrinkages observed in breast MDA-MB-231 and renal 786-O carcinoma models. Pharmacodynamic analyses of the breast model revealed strong reduction in staining of proliferation marker Ki-67 and phosphorylated extracellular regulated kinases 1/2. These data demonstrate that regorafenib is a well-tolerated, orally active multikinase inhibitor with a distinct target profile that may have therapeutic benefit in human malignancies

    Reference

    1. Chu E. An Update on the Current and Emerging Targeted Agents in Metastatic Colorectal Cancer. Clin Colorectal Cancer. 2011 Jul 11. [Epub ahead of print] PubMed PMID: 21752724.

    2. Demetri GD. Differential properties of current tyrosine kinase inhibitors in gastrointestinal stromal tumors. Semin Oncol. 2011 Apr;38 Suppl 1:S10-9. Review.  Erratum in: Semin Oncol. 2011 Jun;38(3):467. PubMed PMID: 21419931.

    3. Wilhelm SM, Dumas J, Adnane L, Lynch M, Carter CA, Schütz G, Thierauch KH, Zopf D. Regorafenib (BAY 73-4506): a new oral multikinase inhibitor of angiogenic, stromal and oncogenic receptor tyrosine kinases with potent preclinical antitumor activity. Int J Cancer. 2011 Jul 1;129(1):245-55. doi: 10.1002/ijc.25864. Epub 2011 Apr 22. PubMed PMID: 21170960.

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