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Formula | C21H15ClF4N4O3.H2O |
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Molecular Weight | 500.83 | CAS No. | 1019206-88-2 | |
Solubility (25°C)* | In vitro | DMSO | 100 mg/mL (199.66 mM) | |
Water | Insoluble | |||
Ethanol | Insoluble | |||
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck 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. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.) |
Description | Regorafenib (BAY-734506, Fluoro-sorafenib, Resihance, Stivarga, regorafaenib monohydrate) Monohydrate is a novel oral multikinase inhibitor with IC50 values of 13, 4.2, 46, 22, 7, 1.5, 2.5, 28, 19 nM for VEGFR1, murine VEGFR2, murine VEGFR3, PDGFR-β, Kit (c-Kit), RET (c-RET), RAF-1, B-RAF and B-RAF(V600E) respectively. | |||||||||||
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Targets |
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In vitro | 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. [1] 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). [2] Regorafenib suppresses growth of human Hep3B, PLC/PRF/5 and HepG2 cells in a concentration- and time-dependent manner. [3] | |||||||||||
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. [1] |
Kinase Assay: |
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Cell Assay: |
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Animal Study: |
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Spatiotemporally resolved colorectal oncogenesis in mini-colons ex vivo [ Nature, 2024, 629(8011):450-457] | PubMed: 38658753 |
Protocol for generation of and high-throughput drug testing with patient-derived colorectal cancer organoids [ STAR Protoc, 2024, 5(2):103090] | PubMed: 38809757 |
Effect of Intraperitoneal Chemotherapy with Regorafenib on IL-6 and TNF-α Levels and Peritoneal Cytology: Experimental Study in Rats with Colorectal Peritoneal Carcinomatosis [ J Clin Med, 2023, 12(23)7267] | PubMed: 38068319 |
Triple MAPK inhibition salvaged a relapsed post-BCMA CAR-T cell therapy multiple myeloma patient with a BRAF V600E subclonal mutation [ J Hematol Oncol, 2022, 15(1):109] | PubMed: 35978321 |
Studies on Biological and Molecular Effects of Small-Molecule Kinase Inhibitors on Human Glioblastoma Cells and Organotypic Brain Slices [ Life (Basel), 2022, 12(8)1258] | PubMed: 36013437 |
Assessment in vitro of interactions between anti-cancer drugs and noncancer drugs commonly used by cancer patients [ Anticancer Drugs, 2022, 10.1097/CAD.0000000000001344] | PubMed: 36066384 |
Regorafenib and reactive metabolite of sunitinib activate inflammasomes: Implications for multi tyrosine kinase inhibitor-Iiduced immune related adverse events [ Pharmazie, 2022, 77(2):54-58] | PubMed: 35209964 |
Impact of a Desmoplastic Tumor Microenvironment for Colon Cancer Drug Sensitivity: A Study with 3D Chimeric Tumor Spheroids [ ACS Appl Mater Interfaces, 2021, 13(41):48478-48491] | PubMed: 34633791 |
Recapitulating cholangiopathy-associated necroptotic cell death in vitro using human cholangiocyte organoids [ Cell Mol Gastroenterol Hepatol, 2021, S2352-345X(21)00223-X] | PubMed: 34700031 |
Leukotriene receptor antagonists enhance HCC treatment efficacy by inhibiting ADAMs and suppressing MICA shedding [ Cancer Immunol Immunother, 2021, 70(1):203-213] | PubMed: 32683508 |
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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.
NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.