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    Regorafenib HCl
    Regorafenib HCl

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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 #: V0071
    CAS #: 835621-07-3 (HCl)Purity ≥98%

    Description: Regorafenib HCl, the hydrochloric acid salt of regorafenib (also known as BAY 73-4506), is a multi-kinase inhibitor which targets 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 is an orally bioavailable small molecule that has anticancer activity and has been approved by FDA for the treatment of liver cancer. Regorafenib strongly prevents VEGFR2 autophosphorylation in NIH-3T3/VEGFR2 cells with IC50 of 3 nM. In HAoSMCs, regorafenib suppress PDGFR-β autophosphorylation after stimulation with PDGF-BB, with an IC50 of 90 nM. It also inhibits FGFR signaling in MCF-7 breast cancer (BC) cells stimulated with FGF10.

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

    Related CAS:755037-03-7 (free base); 1019206-88-2 (Regorafenib monohydrate)

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    Molecular Weight (MW)519.28
    FormulaC₂₁H₁₆Cl₂F₄N₄O₃ 
    CAS No.835621-07-3(HCI)
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: >100 mg/mL (200.9 mM)
    Water: N/A
    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 hydrochloric acid
    SynonymBAY-734506 HCl; BAY 734506; BAY734506; Regorafenib HCl. 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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