Neratinib

Product Description

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.

Solubility

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 all affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:

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Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
0.05 mM	35.90 mL	179.52 mL	359.03 mL
0.25 mM	7.18 mL	35.90 mL	71.81 mL
0.5 mM	3.59 mL	17.95 mL	35.90 mL
2.5 mM	0.72 mL	3.59 mL	7.18 mL

Calculators

Background References

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

• Kwak Irreversible inhibitors of the EGF receptor may circumvent acquired resistance to gefitinib. Proc.Natl.Acad.Sci.U.S.A. 2005 PMID: 15897464
• Yun The T790M mutation in EGFR kinase causes drug resistance by increasing the affinity for ATP. Proc.Natl.Acad.Sci.U.S.A. 2008 PMID: 18227510
• Rabindran Antitumor activity of HKI-272, an orally active, irreversible inhibitor of the HER-2 tyrosine kinase. Cancer Res. 2004 PMID: 15173008