產品名稱：Neratinib, Free Base
產品貨號：LC  N-6404
產品規格：100 MG
Neratinib, also known as HKI-272, is considered to be a second-generation inhibitor of the ErbB family of receptor kinases.  Sequist, L.V., et al.  "Second-Generation Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitors in Non-Small Cell Lung Cancer."  Oncologist 12:  325-330 (2007).
Neratinib is an irreversible inhibitor of the epidermal growth factor receptor (EGFR) and human epidermal growth factor receptor 2 (HER-2) tyrosine kinases by targeting a cysteine residue in the ATP-binding site of the receptor.  Rabindran, S.K., et al.  "Antitumor activity of HKI-272, an orally active, irreversible inhibitor of the HER-2 tyrosine kinase."  Cancer Res. 64:  3958-3965 (2004).
Neratinib inhibits the proliferation of HER-2 overexpressing human breast cancer cell lines and EGFR-dependent cells in vitro.  In vivo, neratinib is active against HER-2- and EGFR-dependent tumor xenograft models.  Rabindran, S.K., et al.  "Antitumor activity of HKI-272, an orally active, irreversible inhibitor of the HER-2 tyrosine kinase."  Cancer Res. 64:  3958-3965 (2004).
Acquired resistance of non-small cell lung cancers to gefitinib because of a T790M mutation in the EGFR kinase domain is circumvented by neratinib.  Kwak, E.L., et al.  "Irreversible inhibitors of the EGF receptor may circumvent acquired resistance to gefitinib."  Proc. Natl. Acad. Sci. USA 102:  7665-7670 (2005).
Neratinib is active against HER-2-positive breast cancer in patients.  Wong, K.K., et al.  "HKI-272, an irreversible pan erbB receptor tyrosine kinase inhibitor: Preliminary phase 1 results in patients with solid tumors."  J. Clin. Oncol. 24:  3018 (2006).
Another CAS number previously assigned to neratinib, namely 736156-77-7, has been deleted by CAS and is no longer in use.
Storage:  Store at or below -20 ºC.  Solubility:  Soluble in DMSO at 2 mg/mL with warming; very poorly soluble in ethanol; very poorly soluble in water; maximum solubility in plain water is estimated to be about 5-20 µM; buffers, serum, or other additives may increase or decrease the aqueous solubility.  Disposal:  A
 

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