An orally active

Neratinib – 1 mg

Brand:
Cayman
CAS:
698387-09-6
Storage:
-20
UN-No:
Non-Hazardous - /

The receptor tyrosine kinase HER2 (ErbB2) is a key component of epidermal growth factor receptor complexes that are known to have central roles in cell proliferation and cancer.{20364,21790} Neratinib is an orally active, irreversible inhibitor of the HER2 kinase (IC50 = 59 nM).{30796} It also potently inhibits several mutants of HER2 and shows 10-fold or greater selectivity over a wide variety of other kinases.{30796,30793,24156} As an irreversible inhibitor, neratinib may circumvent acquired resistance developed against reversible inhibitors, including gefitinib (Item No. 13166).{30795} Neratinib has been evaluated in clinical trials against cancers characterized by HER2 overexpression or HER2 activating mutations.{30794,30797}  

 

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Description

An orally active, irreversible inhibitor of the HER2 kinase (IC50 = 59 nM) that also potently inhibits several mutants of HER2

Formal name: (2E)-N-[4-[[3-chloro-4-(2-pyridinylmethoxy)phenyl]amino]-3-cyano-7-ethoxy-6-quinolinyl]-4-(dimethylamino)-2-butenamide

Synonyms:  HKI-272

Molecular weight: 557

CAS: 698387-09-6

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors|EGFR/ErbB/HER Family||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cancer|Cell Signaling|Growth Factor Receptor Signaling

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