Product Name

Neratinib

General description

Neratinib is a irreversible inhibitor of the HER-2 receptor tyrosine kinase with potential antineoplastic activity, and also a P-Glycoprotein Inhibitor.

Synonym

(E)-N-[4-[3-chloro-4-(pyridin-2-ylmethoxy)anilino]-3-cyano-7-ethoxyquinolin-6-yl]-4-(dimethylamino)but-2-enamide; HKI-272; Nerlynx;

Purity

≥98%(HPLC)

CAS Number

698387-09-6

Formula

C³⁰H²⁹ClN⁶O³

Molecular Weight

557.051

Suitability

BioReagent, suitable for cell culture, etc.

l  Physical and Chemical Information

Appearance

White or Off-white solid

Solubility(25℃)

DMSO

~5mg/mL

Ethanol

Insoluble

Water

Insoluble

l  Biological Information

Biochem/Physiol   Actions

Neratinib is a tyrosine kinase inhibitor   which exhibits antitumor action against Epidermal Growth Factor Receptor (EGFR), HER2, and Human Epidermal Growth Factor Receptor 4 (HER4) postive carcinomas.

Neratinib is an orally available, 6,7-disubstituted-4-anilinoquinoline-3-carbonitrile irreversible inhibitor of the HER-2 receptor tyrosine kinase with potential antineoplastic activity. Neratinib binds to the HER-2 receptor irreversibly, thereby reducing autophosphorylation in cells, apparently by targeting a cysteine residue in the ATP-binding pocket of the receptor. Treatment of cells with this agent results in inhibition of downstream signal transduction events and cell cycle regulatory pathways; arrest at the G1-S (Gap 1/DNA synthesis)-phase transition of the cell division cycle; and ultimately decreased cellular proliferation. Neratinib also inhibits the epidermal growth factor receptor (EGFR) kinase and the proliferation of EGFR-dependent cells.

l  Packaging & Storage

Packaging

10mg; 50mg; 250mg

Storage temp.

0-5℃

l  Precautions and Disclaimer

This   product is for R&D use only, not for drug, household, or other uses.

l  References

1.    http://www.drugbank.ca

2.    https://ncit.nci.nih.gov

3.    https://www.ncbi.nlm.nih.gov