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Submit ReviewWZ 4002
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)
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 Data for WZ 4002
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| 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 | 20.2 mL | 101.01 mL | 202.03 mL |
| 0.5 mM | 4.04 mL | 20.2 mL | 40.41 mL |
| 1 mM | 2.02 mL | 10.1 mL | 20.2 mL |
| 5 mM | 0.4 mL | 2.02 mL | 4.04 mL |
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Product Datasheets for WZ 4002
References for WZ 4002
References are publications that support the biological activity of the product.
Zhou et al (2009) Novel mutant-selective EGFR kinase inhibitors against EGFR T790M. Nature 462 1070 PMID: 20033049
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Keywords: WZ 4002, WZ 4002 supplier, WZ4002, potent, EGFR, epidermal, growth, factor, receptor, tyrosine, kinase, inhibitors, inhibits, mutant-selective, T790M, L858R, 6290, Tocris Bioscience
Citations for WZ 4002
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Literature in this Area
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Angiogenesis in Cancer Poster
This poster summarizes the pathogenesis of angiogenesis in cancer, as well as some of the main angiogenesis therapeutic targets.