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Formula | C21H15ClF4N4O3 |
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Molecular Weight | 482.82 | CAS No. | 755037-03-7 | ||||
Solubility (25°C)* | In vitro | DMSO | 96 mg/mL (198.83 mM) | ||||
Water | Insoluble | ||||||
Ethanol | Insoluble | ||||||
In vivo (Add solvents to the product individually and in order) |
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* <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 is a multi-target inhibitor for VEGFR1, VEGFR2, VEGFR3, PDGFRβ, Kit (c-Kit), RET (c-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 induces autophagy. | |||||||||||
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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 suppresses 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] |
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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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Data from [Data independently produced by , , J Cell Physiol, 2015, 230(9): 2281-98]
Data from [Data independently produced by , , Clin Cancer Res, 2014, 20(22):5768-76]
Data from [Data independently produced by , , Naunyn Schmiedebergs Arch Pharmacol, 2017, 390(11):1125-1134]
Regorafenib plus nivolumab in unresectable hepatocellular carcinoma: the phase 2 RENOBATE trial [ Nat Med, 2024, 10.1038/s41591-024-02824-y] | PubMed: 38374347 |
Spatiotemporally resolved colorectal oncogenesis in mini-colons ex vivo [ Nature, 2024, 629(8011):450-457] | PubMed: 38658753 |
Targeting PDGF signaling of cancer-associated fibroblasts blocks feedback activation of HIF-1α and tumor progression of clear cell ovarian cancer [ Cell Rep Med, 2024, S2666-3791(24)00201-5] | PubMed: 38670097 |
A functional personalised oncology approach against metastatic colorectal cancer in matched patient derived organoids [ NPJ Precis Oncol, 2024, 8(1):52] | PubMed: 38413740 |
Osteosarcoma cells depend on MCL-1 for survival, and osteosarcoma metastases respond to MCL-1 antagonism plus regorafenib in vivo [ BMC Cancer, 2024, 24(1):1350] | PubMed: 39497108 |
Upregulation of LHPP by saRNA inhibited hepatocellular cancer cell proliferation and xenograft tumor growth [ PLoS One, 2024, 19(5):e0299522] | PubMed: 38696452 |
Immuno-oncological effects of standard anticancer agents and commonly used concomitant drugs: an in vitro assessment [ BMC Pharmacol Toxicol, 2024, 25(1):25] | PubMed: 38444002 |
Immuno-oncological effects of standard anticancer agents and commonly used concomitant drugs: an in vitro assessment [ BMC Pharmacol Toxicol, 2024, 25(1):25] | PubMed: 38444002 |
Targeting PSAT1 to mitigate metastasis in tumors with p53-72Pro variant [ Signal Transduct Target Ther, 2023, 8(1):65] | PubMed: 36788227 |
Multiplexed kinase interactome profiling quantifies cellular network activity and plasticity [ Mol Cell, 2023, 83(5):803-818.e8] | PubMed: 36736316 |
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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.
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