Regorafenib (BAY 73-4506)
Catalog No.S1178 Synonyms: Fluoro-Sorafenib
Molecular Weight(MW): 482.82
Regorafenib (BAY 73-4506) is a multi-target inhibitor for VEGFR1, VEGFR2, VEGFR3, PDGFRβ, Kit, RET and Raf-1 with IC50 of 13 nM/4.2 nM/46 nM, 22 nM, 7 nM, 1.5 nM and 2.5 nM in cell-free assays, respectively.
Cited by 13 Publications
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Hepatoma cells 24 h after plating were treated with vehicle (DMSO), regorafenib (REGO, 0.5 µM), PDE5 inhibitor (sildenafil, 2 µM); or the drugs in combination. 24 hours after treatment cells were isolated and viability determined by trypan blue (n=3, SEM). *P 0.05
J Cell Physiol, 2015, 230(9): 2281-98. Regorafenib (BAY 73-4506) purchased from Selleck.
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|Description||Regorafenib (BAY 73-4506) is a multi-target inhibitor for VEGFR1, VEGFR2, VEGFR3, PDGFRβ, Kit, RET and Raf-1 with IC50 of 13 nM/4.2 nM/46 nM, 22 nM, 7 nM, 1.5 nM and 2.5 nM in cell-free assays, respectively.|
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. Regorafenib also inhibits FGFR signaling in MCF-7 breast cancer (BC) cells stimulated with FGF10. Regorafenib very potently inhibited the mutant receptors KITK642E and RETC634W, with IC50 of approximately 20 nM and 10 nM, respectively. Regorafenib inhibits the proliferation of VEGF165-stimulated HUVECs, with an IC50 of approximately 3 nM. Regorafenib prevents the proliferation of FGF2-stimulated HUVECs and of PDGF-BB-stimulated HAoSMCs with IC50 of 127 nM and 146 nM, respectively.  Regorafenib 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).  Regorafenib suppresses growth of human Hep3B, PLC/PRF/5 and HepG2 cells in a concentration- and time-dependent manner. 
|In vivo||Regorafenib 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. |
Kinase assays:In vitro assays using recombinant VEGFR2 (murine aa785–aa1367), VEGFR3 (murine aa818–aa1363), PDGFRβ (aa561–aa1106), Raf-1 (aa305–aa648) and BRafV600E (aa409–aa765) kinase domains are performed. Initial in vitro kinase inhibition profiling is performed at a fixed 1 μM Regorafenib concentration. Inhibitory concentration of 50% (IC50) values are determined from selected responding kinases, e.g., VEGFR1 and RET. TIE2 kinase inhibition is measured with a homogeneous time-resolved fluorescence (HTRF) assay using a recombinant fusion protein of glutathione-S-transferase, the intracellular domain of TIE2 and the peptide biotin-Ahx-EPKDDAYPLYSDFG as substrate.
|In vitro||DMSO||97 mg/mL (200.9 mM)|
|In vivo||30% PEG400+0.5% Tween80+5% propylene glycol||30 mg/mL|
* 1 mg/ml means slightly soluble or insoluble.
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Clinical Trial Information
|NCT Number||Recruitment||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT02795156||Recruiting||Non-small Cell Lung Carcinoma|Urothelial Carcinoma|Gastrointestinal Carcinoma, Non-colon|Upper Aerodigestive Tract Carcinoma||SCRI Development Innovations, LLC|Foundation Medicine|Boehringer Ingelheim|Bayer||September 28, 2016||Phase 2|
|NCT03042689||Not yet recruiting||Acute Myeloid Leukemia||Massachusetts General Hospital|Bayer||January 2017||Phase 1|
|NCT02910843||Not yet recruiting||Rectal Cancer||Swiss Group for Clinical Cancer Research||December 2016||Phase 1|
|NCT02940223||Not yet recruiting||Malignant Neoplasms of Independent (Primary) Multiple Sites|Metastatic Colorectal Cancer||M.D. Anderson Cancer Center|Bayer||December 2016||Phase 2|
|NCT02955940||Enrolling by invitation||Pancreatic Cancer|Colorectal Cancer|Breastcancer|Lung Cancer Non-Small Cell||Incyte Corporation||November 2016||Phase 2|
|NCT02889328||Recruiting||Gastrointestinal Stromal Tumors (GISTs)||Asan Medical Center||September 2016||Phase 2|
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