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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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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F1502104 | Certificate of Analysis | Jan 25, 2023 | R127804 |
A2305736 | Certificate of Analysis | Nov 10, 2022 | R127804 |
A2305737 | Certificate of Analysis | Nov 10, 2022 | R127804 |
A2305740 | Certificate of Analysis | Nov 10, 2022 | R127804 |
A2305809 | Certificate of Analysis | Nov 10, 2022 | R127804 |
A2305815 | Certificate of Analysis | Nov 10, 2022 | R127804 |
A2305850 | Certificate of Analysis | Nov 10, 2022 | 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. 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] |
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:] |