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Neratinib is an irreversible EGFR inhibitor that displays anticancer chemotherapeutic benefit in the treatment of HER2 positive breast cancers and non-small cell lung cancer (NSCLC). Neratinib prevents ligand-induced receptor dimerization by targeting a cysteine residue in the ATP binding pocket of the receptor. In pre-clinical models, this compound induces cell cycle arrest and decreases cell proliferation.
| Cas No. | 698387-09-6 |
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| Purity | ≥98% |
| Formula | C30H29ClN6O3 |
| Formula Wt. | 557.04 |
| Chemical Name | (2E)-N-[4-[[3-chloro-4-[(pyridin-2-yl)methoxy]phenyl]amino]-3-cyano-7-ethoxyquinolin-6-yl]-4-(dimethylamino)but-2-enamide |
| IUPAC Name | (E)-N-[4-[3-chloro-4-(pyridin-2-ylmethoxy)anilino]-3-cyano-7- ethoxyquinolin-6-yl]-4-(dimethylamino)but-2-enamide |
| Synonym | HKI-272, WAY-179272 |
| Appearance | Off white to slight yellow powder |
| Store Temp | Ambient |
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| Ship Temp | Ambient |
| MSDS | |
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| Info Sheet |
López-Tarruella S, Jerez Y, Márquez-Rodas I, et al. Neratinib (HKI-272) in the treatment of breast cancer. Future Oncol. 2012 Jun;8(6):671-81. PMID: 22764764.
Sánchez-Martín M, Pandiella A. Differential action of small molecule HER kinase inhibitors on receptor heterodimerization: therapeutic implications. Int J Cancer. 2012 Jul 1;131(1):244-52. PMID: 21826647.
Wong KK, Fracasso PM, Bukowski RM, et al. A phase I study with neratinib (HKI-272), an irreversible pan ErbB receptor tyrosine kinase inhibitor, in patients with solid tumors. Clin Cancer Res. 2009 Apr 1;15(7):2552-8. PMID: 19318484.
Rabindran SK, Discafani CM, Rosfjord EC, et al. Antitumor activity of HKI-272, an orally active, irreversible inhibitor of the HER-2 tyrosine kinase. Cancer Res. 2004 Jun 1;64(11):3958-65. PMID: 1517300.