Determine the necessary mass, volume, or concentration for preparing a solution.
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
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SKU | Size | Availability | Price | Qty |
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R127804-5mg | 5mg | Available within 4-8 weeks(?) Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience! | $35.90 | |
R127804-10mg | 10mg | Available within 4-8 weeks(?) Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience! | $58.90 | |
R127804-25mg | 25mg | In stock | $132.90 | |
R127804-100mg | 100mg | In stock | $177.90 | |
R127804-500mg | 500mg | In stock | $801.90 |
Potent multikinase inhibitor
Synonyms | CCG-269571 | AB00076187-01 | CHEBI:68647 | 755037-03-7 , Regorafenib | AC-25075 | MFCD16038047 | Regorafenib,BAY 73-4506 | 4-[4-({[4-Chloro-3-(trifluoromethy)phenyl]carbamoyl}amino)-3-fluorophenoxy]-1-methylpyridine-2-carboxamide | 2-Pyridinecarboxamide,4 |
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Specifications & Purity | Moligand™, ≥99% |
Biochemical and Physiological Mechanisms | Potent\xa0multikinase inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFRβ, c-Kit, RET and Raf-1 (IC 50 values are 13, 4.2, 46, 22, 7, 1.5 and 2.5nM, respectively). Orally bioavailable antitumor, antiangiogenic, antiproliferative and antineoplastic agent. |
Storage Temp | Store at -20°C |
Shipped In | Ice chest + Ice pads |
Grade | Moligand™ |
Action Type | INHIBITOR |
Mechanism of action | Nerve growth factor receptor Trk-A |
Product 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, respectively. |
ALogP | 4.2 |
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Mechanism of Action | Action Type | target ID | Target Name | Target Type | Target Organism | Binding Site Name | References |
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IUPAC Name | 4-[4-[[4-chloro-3-(trifluoromethyl)phenyl]carbamoylamino]-3-fluorophenoxy]-N-methylpyridine-2-carboxamide |
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INCHI | InChI=1S/C21H15ClF4N4O3/c1-27-19(31)18-10-13(6-7-28-18)33-12-3-5-17(16(23)9-12)30-20(32)29-11-2-4-15(22)14(8-11)21(24,25)26/h2-10H,1H3,(H,27,31)(H2,29,30,32) |
InChi Key | FNHKPVJBJVTLMP-UHFFFAOYSA-N |
Canonical SMILES | CNC(=O)C1=NC=CC(=C1)OC2=CC(=C(C=C2)NC(=O)NC3=CC(=C(C=C3)Cl)C(F)(F)F)F |
Isomeric SMILES | CNC(=O)C1=NC=CC(=C1)OC2=CC(=C(C=C2)NC(=O)NC3=CC(=C(C=C3)Cl)C(F)(F)F)F |
PubChem CID | 11167602 |
Molecular Weight | 482.82 |
PubChem CID | 11167602 |
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CAS Registry No. | 755037-03-7 |
ChEMBL Ligand | CHEMBL1946170 |
ChEBI | CHEBI:68647 |
Wikipedia | Regorafenib |
DrugBank Ligand | DB08896 |
PEP | regorafenib |
Reactome Reaction | R-HSA-6802938, R-HSA-9669854, R-HSA-9669900, R-HSA-9674430, R-HSA-9674095, R-HSA-9669870, R-HSA-9674408 |
Reactome Drug | R-ALL-9657514 |
DrugCentral Ligand | 4654 |
Enter Lot Number to search for COA:
Find and download the COA for your product by matching the lot number on the packaging.
Lot Number | Certificate Type | Date | Item |
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A2305809 | Certificate of Analysis | Oct 17, 2024 | R127804 |
A2305737 | Certificate of Analysis | Oct 17, 2024 | R127804 |
A2305736 | Certificate of Analysis | Oct 17, 2024 | R127804 |
A2305740 | Certificate of Analysis | Oct 10, 2024 | R127804 |
A2305815 | Certificate of Analysis | Oct 10, 2024 | R127804 |
A2305850 | Certificate of Analysis | Oct 10, 2024 | R127804 |
F1502104 | Certificate of Analysis | Jan 25, 2023 | R127804 |
H1814073 | Certificate of Analysis | May 09, 2022 | R127804 |
H1814072 | Certificate of Analysis | May 09, 2022 | R127804 |
G1806033 | Certificate of Analysis | Apr 14, 2022 | R127804 |
Solubility | DMSO ≥95mg/mL;Water <1 mg/mL;Ethanol <1 mg/mL |
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Sensitivity | Heat Sensitive |
Melt Point(°C) | 208 °C |
Pictogram(s) | GHS08, GHS09, GHS07 |
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Signal | Danger |
Hazard Statements | H302:Harmful if swallowed H400:Very toxic to aquatic life H410:Very toxic to aquatic life with long lasting effects H372:Causes damage to organs through prolonged or repeated exposure H360:May damage fertility or the unborn child H362:May cause harm to breast-fed children |
Precautionary Statements | P273:Avoid release to the environment. P280:Wear protective gloves/protective clothing/eye protection/face protection. P405:Store locked up. P501:Dispose of contents/container to ... P264:Wash hands [and …] thoroughly after handling. P260:Do not breathe dust/fume/gas/mist/vapors/spray. P270:Do not eat, drink or smoke when using this product. P391:Collect spillage. P330:Rinse mouth. P263:Avoid contact during pregnancy/while nursing. P203:Obtain, read and follow all safety instructions before use. P301+P317:IF SWALLOWED: Get medical help. P318:if exposed or concerned, get medical advice. P319:Get medical help if you feel unwell. |
1. Hang Hu, Defeng Xu. (2022) pH-Sensitive nanoparticles co-loaded with dimethylcurcumin and regorafenib for targeted combinational therapy of hepatocellular carcinoma. EUROPEAN POLYMER JOURNAL, 177 (111434). [PMID:] [10.1016/j.eurpolymj.2022.111434] |
2. Tianfeng Yang, Jian Huo, Rui Xu, Yanmin Zhang. (2021) Synergistic effect of toosendanin and regorafenib against cell proliferation and migration by regulating WWOX signaling pathway in hepatocellular carcinoma. PHYTOTHERAPY RESEARCH, 35 (8): (4567-4578). [PMID:34058790] [10.1002/ptr.7174] |
3. Ruobing Wang, Yahui Liu, Xuguang Mi, Qingmin Chen, Peiqiang Jiang, Junjie Hou, Yifan Lin, Siqi Li, Bai Ji, Yanqiu Fang. (2020) Sirt3 promotes hepatocellular carcinoma cells sensitivity to regorafenib through the acceleration of mitochondrial dysfunction. ARCHIVES OF BIOCHEMISTRY AND BIOPHYSICS, 689 (108415). [PMID:32562663] [10.1016/j.abb.2020.108415] |
1. Hafner FT, Werner D, Kaiser M. (2014) Determination of regorafenib (BAY 73-4506) and its major human metabolites BAY 75-7495 (M-2) and BAY 81-8752 (M-5) in human plasma by stable-isotope dilution liquid chromatography-tandem mass spectrometry.. Bioanalysis, 6 (14): (1923-37). [PMID:25158964] [10.1021/op500134e] |
2. Hang Hu, Defeng Xu. (2022) pH-Sensitive nanoparticles co-loaded with dimethylcurcumin and regorafenib for targeted combinational therapy of hepatocellular carcinoma. EUROPEAN POLYMER JOURNAL, 177 (111434). [PMID:] [10.1016/j.eurpolymj.2022.111434] |
3. Tianfeng Yang, Jian Huo, Rui Xu, Yanmin Zhang. (2021) Synergistic effect of toosendanin and regorafenib against cell proliferation and migration by regulating WWOX signaling pathway in hepatocellular carcinoma. PHYTOTHERAPY RESEARCH, 35 (8): (4567-4578). [PMID:34058790] [10.1002/ptr.7174] |
4. Ruobing Wang, Yahui Liu, Xuguang Mi, Qingmin Chen, Peiqiang Jiang, Junjie Hou, Yifan Lin, Siqi Li, Bai Ji, Yanqiu Fang. (2020) Sirt3 promotes hepatocellular carcinoma cells sensitivity to regorafenib through the acceleration of mitochondrial dysfunction. ARCHIVES OF BIOCHEMISTRY AND BIOPHYSICS, 689 (108415). [PMID:32562663] [10.1016/j.abb.2020.108415] |