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    Regorafenib (BAY73-4506)
    Regorafenib (BAY73-4506)

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V0048
    CAS #: 755037-03-7Purity ≥98%

    Description: Regorafenib (also known as BAY 73-4506; BAY-73-4506) is a potent and orally bioavailable multi-kinase inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFRβ, Kit, RET and Raf-1 with IC50 values of 13 nM/4.2 nM/46 nM, 22 nM, 7 nM, 1.5 nM and 2.5 nM in cell-free assays, respectively. It has antitumor activity and was approved by FDA for the treatment of liver cancer.

    References:  Int J Cancer, 2011, 129(1), 245-255.

    Related CAS: 835621-07-3 (HCl); 1019206-88-2 (Regorafenib monohydrate); 835621-11-9 (Regorafénib N-oxyde Metabolite M2)

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    • 香港大学
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    Molecular Weight (MW)482.82
    CAS No.755037-03-7
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 97 mg/mL (200.9 mM)
    Water:<1 mg/mL (slightly soluble or insoluble)
    Ethanol: N/A
    Solubility (In vivo)30% PEG400+0.5% Tween80+5% Propylene glycol: 30mg/mL
    Chemical Name1-(4-chloro-3-(trifluoromethyl)phenyl)-3-(2-fluoro-4-(2-(methylcarbamoyl)pyridin-4-yloxy)phenyl)urea
    SynonymBAY-734506; BAY 734506; BAY734506; Regorafenib. Brand name: Stivarga.
    SMILES CodeO=C(NC1=CC=C(C(C(F)(F)F)=C1)Cl)NC2=CC=C(OC3=CC(C(NC)=O)=NC=C3)C=C2F.O

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    In VitroRegorafenib targets both tumor cell proliferation and tumor vasculature through inhibition of receptors of tyrosine kinases (VEGFR, KIT, RET, FGFR, and PDGFR) and serine/threonine kinases (Raf and p38MAPK).
    In VivoRegorafenib reveals potent dose-dependent TGI in various preclinical human xenograft models in mice, with tumor shrinkages in breast MDA-MB-231 and renal 786-O carcinoma models. Regorafenib prevents not only the growth of syngeneic primary 4T1 breast tumors growing orthotopically in the fat pad, but also suppresses the formation of tumor metastasis in the lung.
    Animal modelFemale athymic NCr nu/nu mice with Colo-205, MDA-MB-231 or 786-O
    Formulation & DosagePEG400/125 mM aqueous methanesulfonic acid (80/20) or polypropylene glycol/PEG400/Pluronic F68 (42.5/42.5/15 + 20% Aqua); 3, 10, 30, 200 mg/kg; oral
    References[1] Wilhelm SM, et al. Int J Cancer, 2011, 129(1), 245-255.

    These protocols are for reference only. InvivoChem does not independently validate these methods.

    Regorafenib (BAY 73-4506)

    Regorafenib inhibits growth-factor-stimulated VEGFR2 and VEGFR3 autophosphorylation in human umbilical vascular endothelialcells (HuVECs) and intracellular signaling and migration in lymphatic endothelial cells (LECs).

    Regorafenib (BAY 73-4506)

    Regorafenib inhibits key kinase targets in cells expressing VEGFR2, TIE2, PDGFR‐β, or FGFR.   2011 Jul 1;129(1):245-55.


    Regorafenib (BAY 73-4506)

    Regorafenib inhibits tumor vasculature and tumor growth in a rat GS9L glioblastoma model: time‐course analysis by DCE‐MRI.   2011 Jul 1;129(1):245-55.

    Regorafenib (BAY 73-4506)

    Regorafenib significantly reduces tumor MVA in the Colo‐205 CRC xenograft model.  2011 Jul 1;129(1):245-55.


    Regorafenib (BAY 73-4506)

    Regorafenib exhibits antitumorigenic and antiangiogenic effects in the MDA‐MB‐231 breast xenograft model.  2011 Jul 1;129(1):245-55.


    Regorafenib (BAY 73-4506)

    In vivo antitumor efficacy of regorafenib.  2011 Jul 1;129(1):245-55.


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