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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
|Storage||Store at -20°C|
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|
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.
|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|
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
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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
Citations are publications that use Tocris products.
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Literature in this Area
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