WZ 4002

Name: WZ 4002
Brand: Tocris Bioscience
SKU: 6290

Tocris Bioscience, part of Bio-Techne | Catalog # 6290

COA / SDS

Potent mutant-selective EGFR inhibitor

Key Product Details

Description:	Potent mutant-selective EGFR inhibitor
Chemical Name:	N-[3-[[5-Chloro-2-[[2-methoxy-4-(4-methyl-1-piperazinyl)phenyl]amino]-4-pyrimidinyl]oxy]phenyl]-2-propenamide
Purity:	≥98% (HPLC)
Molecular Weight:	494.98

View Full Technical Details for WZ 4002

Technical Data
Citations

Biological Activity for WZ 4002

WZ 4002 is a potent irreversible mutant selective EGFR tyrosine kinase inhibitor. It blocks ATP-dependent autophosphorylation of EGFR carrying the T790M or L858R mutation (IC₅₀ = 8 nM). WZ 4002 exhibits selectivity for mutant EGFR over wild-type. In mice bearing T790M mutant lung cancer cell lines WZ 4002 inhibits EGFR, AKT and ERK1/2 phosphorylation and results in significant tumor regression.

Licensing Information

Sold under license from Dana-Farber Cancer Institute.

Technical Data for WZ 4002

M. Wt	494.98
Formula	C₂₅H₂₇ClN₆O₃
Storage	Store at -20°C
Purity	≥98% (HPLC)
CAS Number	1213269-23-8
PubChem ID	44607530
InChi Key	ITTRLTNMFYIYPA-UHFFFAOYSA-N
Smiles	COC1=C(NC2=NC=C(Cl)C(OC3=CC(NC(C=C)=O)=CC=C3)=N2)C=CC(N4CCN(C)CC4)=C1

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 WZ 4002

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
Solubility	DMSO	4.95	10

Preparing Stock Solutions for WZ 4002

The following data is based on the product molecular weight 494.98.

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
0.1 mM	20.20 mL	101.01 mL	202.03 mL
0.5 mM	4.04 mL	20.20 mL	40.41 mL
1 mM	2.02 mL	10.10 mL	20.20 mL
5 mM	0.40 mL	2.02 mL	4.04 mL

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References for WZ 4002

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

Zhou Novel mutant-selective EGFR kinase inhibitors against EGFR T790M. Nature 2009 PMID: 20033049