Neratinib

Name: Neratinib
Brand: Tocris Bioscience
SKU: 7371

Tocris Bioscience, part of Bio-Techne | Catalog # 7371

Citations (2)

COA / SDS

Potent HER2 receptor tyrosine kinase and EGFR kinase inhibitor

Key Product Details

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)
Molecular Weight:	557.05

View Full Technical Details for Neratinib

Technical Data
Citations

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
InChi Key	JWNPDZNEKVCWMY-VQHVLOKHSA-N
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 for Neratinib

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
Solubility	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.

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

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References for Neratinib

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