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Description: Potent HER2 receptor tyrosine kinase and EGFR kinase inhibitor
Chemical Name: (2E)-N-[4-[[3-Chloro-4-(2-pyridinylmethoxy)phenyl]amino]-3-cyano-7-ethoxy-6-quinolinyl]-4-(dimethylamino)-2-butenamide
Purity: ≥98% (HPLC)
Literature (1)

Biological Activity for Neratinib

Neratinib is a potent, irreversible inhibitor of HER-2/ErbB2 receptor tyrosine kinase and EGFR kinase (IC50 = 59 nM and 92 nM, respectively). Neratinib reduces receptor autophosphorylation and proliferation of EGFR-dependent cancer cells, blocks cell-cycle progression and inhibits HER-2 signaling pathways. Neratinib suppresses proliferation of gefitinib-resistant non-small cell lung cancer cells expressing mutant EGFR. Also inhibits MST1 (IC50 = 37.7 nM). Orally bioavailable.

Technical Data for Neratinib

M. Wt 557.05
Formula C30H29ClN6O3
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 698387-09-6
PubChem ID 9915743
Smiles N(C=1C2=C(C=C(OCC)C(NC(/C=C/CN(C)C)=O)=C2)N=CC1C#N)C3=CC(Cl)=C(OCC4=CC=CC=N4)C=C3

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data for Neratinib

Solvent Max Conc. mg/mL Max Conc. mM
DMSO 2.79 5

Preparing Stock Solutions for Neratinib

The following data is based on the product molecular weight 557.05. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
0.05 mM 35.9 mL 179.52 mL 359.03 mL
0.25 mM 7.18 mL 35.9 mL 71.81 mL
0.5 mM 3.59 mL 17.95 mL 35.9 mL
2.5 mM 0.72 mL 3.59 mL 7.18 mL

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References for Neratinib

References are publications that support the biological activity of the product.

Rabindran et al (2004) Antitumor activity of HKI-272, an orally active, irreversible inhibitor of the HER-2 tyrosine kinase. Cancer Res. 64 3958 PMID: 15173008

Kwak et al (2005) Irreversible inhibitors of the EGF receptor may circumvent acquired resistance to gefitinib. Proc.Natl.Acad.Sci.U.S.A. 102 7665 PMID: 15897464

Yun et al (2008) The T790M mutation in EGFR kinase causes drug resistance by increasing the affinity for ATP. Proc.Natl.Acad.Sci.U.S.A. 105 2070 PMID: 18227510

If you know of a relevant reference for Neratinib, please let us know.

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Keywords: Neratinib, Neratinib supplier, potent, irreversible, HER2, ERBB2, tyrosine, kinase, inhibitors, inhibitory, inhibition, EGFR, epidermal, growth, factor, receptor, MST1, Other, Kinases, 7371, Tocris Bioscience

Citations for Neratinib

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Literature in this Area

Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!

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Angiogenesis in Cancer Poster

Angiogenesis in Cancer Poster

This poster summarizes the pathogenesis of angiogenesis in cancer, as well as some of the main angiogenesis therapeutic targets.