Customization: | Available |
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Powder: | Yes |
Customized: | Customized |
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Product Name | Neratinib |
Appearance | White to off-white powder |
CAS No. | 698387-09-6 |
MF | C30H29ClN6O3 |
MW | 557.04 |
Function:
1. It is a tyrosine kinase inhibitor.
2. It has been used in extended adjuvant therapy for early HER2 positive breast cancer.
Application
The receptor tyrosine kinase HER2 (ErbB2) is a key component of epidermal grow factor receptor complexes that are known to have central roles in cell proliferation and cancer. Neratinib is an orally active, irreversible inhibitor of the HER2 kinase (IC50 = 59 nM). It also potently inhibits several mutants of HER2 and shows 10-fold or greater selectivity over a wide variety of other kinases. As an irreversible inhibitor, neratinib may circumvent acquired resistance developed against reversible inhibitors, including gefiti nib . Neratinib has been evaluated in clinical trials against cancers characterized by HER2 overexpression or HER2 activating mutations.