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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P125444-1mg | 1mg | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $13.90 | |
P125444-5mg | 5mg | Available within 4-8 weeks(?) Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience! | $53.90 | |
P125444-25mg | 25mg | Available within 4-8 weeks(?) Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience! | $129.90 | |
P125444-100mg | 100mg | Available within 4-8 weeks(?) Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience! | $238.90 |
Irreversible EGFR inhibitor
Synonyms | EKB-569 | Glyoxylic acid, 2-(dimethyl acetal) | (E)-N-(4-(3-chloro-4-fluorophenylamino)-3-cyano-7-ethoxyquinolin-6-yl)-4-(dimethylamino)but-2-enamide | X5DWL380Z6 | UNII-X5DWL380Z6 | 1-(2-hydroxy-4,6-dimethoxy-phenyl)ethanone | 4-chloro-2-amino-benzoic ac |
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Specifications & Purity | Moligand™, ≥98% |
Biochemical and Physiological Mechanisms | Pelitinib is a tyrosine kinase inhibitor that covalently binds to EGFR, inhibiting receptor phosphorylation and thus inhibiting signal transduction from EGFR. This induces apoptosis and thus leads to suppression of growth in tumor cell lines.Irreversible |
Storage Temp | Store at -20°C |
Shipped In | Ice chest + Ice pads |
Grade | Moligand™ |
Action Type | INHIBITOR |
Mechanism of action | Epidermal growth factor receptor erbB1 inhibitor |
Note | Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20°C. Generally, these will be useable for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour. Need more advice on solubility, usage and handling? Please visit our frequently asked questions (FAQ) page for more details. |
Product Description | Pelitinib (EKB-569) is a potent irreversible EGFR inhibitor with IC50 of 38.5 nM. |
ALogP | 4.5 |
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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 | (E)-N-[4-(3-chloro-4-fluoroanilino)-3-cyano-7-ethoxyquinolin-6-yl]-4-(dimethylamino)but-2-enamide |
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INCHI | InChI=1S/C24H23ClFN5O2/c1-4-33-22-12-20-17(11-21(22)30-23(32)6-5-9-31(2)3)24(15(13-27)14-28-20)29-16-7-8-19(26)18(25)10-16/h5-8,10-12,14H,4,9H2,1-3H3,(H,28,29)(H,30,32)/b6-5+ |
InChi Key | WVUNYSQLFKLYNI-AATRIKPKSA-N |
Canonical SMILES | CCOC1=C(C=C2C(=C1)N=CC(=C2NC3=CC(=C(C=C3)F)Cl)C#N)NC(=O)C=CCN(C)C |
Isomeric SMILES | CCOC1=C(C=C2C(=C1)N=CC(=C2NC3=CC(=C(C=C3)F)Cl)C#N)NC(=O)/C=C/CN(C)C |
WGK Germany | 3 |
PubChem CID | 6445562 |
Molecular Weight | 467.92 |
PubChem CID | 6445562 |
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CAS Registry No. | 257933-82-7 |
ChEBI | CHEBI:38927 |
ChEMBL Ligand | CHEMBL607707 |
RCSB PDB Ligand | 93J |
Reactome Reaction | R-HSA-1220611, R-HSA-1225978 |
Reactome Drug | R-ALL-1216524 |
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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G1521060 | Certificate of Analysis | Feb 03, 2023 | P125444 |
Solubility | Soluble in DMSO (13 mg/ml at 25 °C), methanol, water (<1 mg/ml at 25 °C), and ethanol (<1 mg/ml at 25 °C). |
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Sensitivity | Light Sensitive,Heat Sensitive |
Melt Point(°C) | 198 °C |
Pictogram(s) | GHS06 |
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Signal | Danger |
Hazard Statements | H301:Toxic if swallowed |
Precautionary Statements | P321:Specific treatment (see ... on this label). P405:Store locked up. P501:Dispose of contents/container to ... P264:Wash hands [and …] thoroughly after handling. P270:Do not eat, drink or smoke when using this product. P330:Rinse mouth. P301+P316:IF SWALLOWED: Get emergency medical help immediately. |
WGK Germany | 3 |