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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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N126132-5mg | 5mg | Available within 4-8 weeks(?) Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience! | $19.90 | |
N126132-25mg | 25mg | Available within 4-8 weeks(?) Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience! | $81.90 | |
N126132-100mg | 100mg | Available within 4-8 weeks(?) Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience! | $162.90 |
Synonyms | EC 244-343-6 | N-(4-(3-chloro-4-(pyridin-2-ylmethoxy)phenylamino)-3-cyano-7-ethoxyquinolin-6-yl)-4-(dimethylamino)butanamide | CHEBI:61397 | N-(4-(3-chloro-4-(pyridin-2-ylmethoxy)phenylamino)-3-cyano-7-ethoxyquinolin-6-yl)-4-(dimethylamino)but-2-enamide | |
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Specifications & Purity | Moligand™, ≥99% |
Biochemical and Physiological Mechanisms | Neratinib is a potent and selective inhibitor of EGFR and Neu(HER2) (IC50 = 92 nM and 59 nM, respectively) by preventing phosphorylation of these proteins by their respective kinases. Neratinib displays activity against a variety of cancer cell lines, inc |
Storage Temp | Store at -20°C |
Shipped In | Ice chest + Ice pads |
Grade | Moligand™ |
Action Type | INHIBITOR |
Mechanism of action | Receptor protein-tyrosine kinase erbB-4 inhibitor |
Product Description | Neratinib (HKI-272) is a highly selective HER2 and EGFR inhibitor with IC50 of 59 nM and 92 nM; weakly inhibits KDR and Src, no significant inhibition to Akt, CDK1/2/4, IKK-2, MK-2, PDK1, c-Raf and c-Met. Phase 3. |
ALogP | 4.9 |
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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-(pyridin-2-ylmethoxy)anilino]-3-cyano-7-ethoxyquinolin-6-yl]-4-(dimethylamino)but-2-enamide |
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INCHI | InChI=1S/C30H29ClN6O3/c1-4-39-28-16-25-23(15-26(28)36-29(38)9-7-13-37(2)3)30(20(17-32)18-34-25)35-21-10-11-27(24(31)14-21)40-19-22-8-5-6-12-33-22/h5-12,14-16,18H,4,13,19H2,1-3H3,(H,34,35)(H,36,38)/b9-7+ |
InChi Key | JWNPDZNEKVCWMY-VQHVLOKHSA-N |
Canonical SMILES | CCOC1=C(C=C2C(=C1)N=CC(=C2NC3=CC(=C(C=C3)OCC4=CC=CC=N4)Cl)C#N)NC(=O)C=CCN(C)C |
Isomeric SMILES | CCOC1=C(C=C2C(=C1)N=CC(=C2NC3=CC(=C(C=C3)OCC4=CC=CC=N4)Cl)C#N)NC(=O)/C=C/CN(C)C |
PubChem CID | 9915743 |
Molecular Weight | 557.04 |
CAS Registry No. | 698387-09-6 |
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Wikipedia | Neratinib |
DiscoveRx TREEspot | HKI-272| |
PubChem CID | 9915743 |
ChEMBL Ligand | CHEMBL180022 |
Reactome Reaction | R-HSA-1220611, R-HSA-1225978, R-HSA-9652264, R-HSA-9665412, R-HSA-9665121, R-HSA-9665702, R-HSA-9665286 |
Reactome Drug | R-ALL-1216527 |
DrugCentral Ligand | 5252 |
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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C1518027 | Certificate of Analysis | Jul 08, 2024 | N126132 |
Solubility | Soluble in DMSO (2 mg/ml at 25 °C), water (<1 mg/ml at 25 °C), and ethanol (<1 mg/ml at 25 °C). |
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1. Rabindran SK, Discafani CM, Rosfjord EC, Baxter M, Floyd MB, Golas J, Hallett WA, Johnson BD, Nilakantan R, Overbeek E et al.. (2004) Antitumor activity of HKI-272, an orally active, irreversible inhibitor of the HER-2 tyrosine kinase.. Cancer Res, 64 (11): (3958-65). [PMID:15173008] [10.1021/op500134e] |
2. Park JW, Liu MC, Yee D, Yau C, van 't Veer LJ, Symmans WF, Paoloni M, Perlmutter J, Hylton NM, Hogarth M et al.. (2016) Adaptive Randomization of Neratinib in Early Breast Cancer.. N Engl J Med, 375 (1): (11-22). [PMID:27406346] [10.1021/op500134e] |