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WZ4002

Catalog No. T6238   CAS 1213269-23-8

WZ4002 is a mutant-selective EGFR inhibitor for EGFR(L858R) and EGFR(T790M) with IC50 of 2 nM/8 nM.

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WZ4002 Chemical Structure
WZ4002, CAS 1213269-23-8
Pack Size Availability Price/USD Quantity
5 mg In stock $ 46.00
10 mg In stock $ 67.00
25 mg In stock $ 119.00
50 mg In stock $ 197.00
100 mg In stock $ 347.00
200 mg In stock $ 516.00
1 mL * 10 mM (in DMSO) In stock $ 52.00
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Purity: 98.12%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description WZ4002 is a mutant-selective EGFR inhibitor for EGFR(L858R) and EGFR(T790M) with IC50 of 2 nM/8 nM.
Targets&IC50 EGFR (L858R):2 nM, EGFR (L858R/T790M):8 nM
In vitro WZ4002 inhibits other EGFR genotypes E746_A750 and E746_A750/T790M with IC50 of 2 and 6 nM. Besides, WZ4002 suppresses widetype ERBB2 with an IC50 of 32 nM. WZ4002 inhibits EGFR, AKT and ERK1/2 phosphorylation in NSCLC cell lines and WZ4002 prevents of EGFR phosphorylation in NIH-3T3 cells expressing different EGFR T790M mutant alleles. For WZ4002, kinases that exhibited greater than 95% inhibition relative to the DMSO control at 10 μM are selected for measurement of their dissociation constants. WZ4002, which possesses an ortho-methoxy group at the C2-aniline substituent, is more selective for EGFR compared to WZ3146. WZ4002 is 100-fold less effective at inhibiting phosphorylation of WT EGFR compared to the quinazoline inhibitors. Similarly, WZ4002 prevents EGFR kinase activity of recombinant L858R/T790M protein more potently than of WT EGFR, while the opposite is observed with HKI-272 and gefitinib. [1] In addition, the phosphorylated EGFR of Src TKI-resistant H1975 cells, as well as HCC827 cells, is completely suppressed by the third generation EGFR TKI, WZ4002. [2]
In vivo In a 2-week efficacy study, WZ4002 treatment results in significant tumor regressions compared to vehicle alone in both T790M containing murine models. [1] Treatment with low-dose WZ4002, and high-dose WZ4002 leads to mean decreases in tracer uptake of 26%, and 36%, respectively. [3]
Kinase Assay EGFR kinase assays: In vitro inhibitory enzyme kinetic assays using recombinant EGFR L858R/T790M and WT protein and are performed using the ATP/NADH coupled assay system in a 96-well format. WZ4002 is added to determine its inhibitory effects.
Cell Research The NSCLC, Ba/F3 cells, NIH-3T3 cells, PC9 gR4 cells are used and verified to contain EGFR delE746_A750/T790M by direct sequencing. Cell proliferation and growth assays are performed using the MTS assay. Site directed mutagenesis is performed using the Quick Change Site-Directed Mutagenesis kit.(Only for Reference)
Molecular Weight 494.97
Formula C25H27ClN6O3
CAS No. 1213269-23-8

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

H2O: < 1 mg/mL (insoluble or slightly soluble)

DMSO: 11 mg/mL (22.3 mM)

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

TargetMolReferences and Literature

1. Zhou W, et al. Nature. 2009, 462(7276), 1070-1074. 2. Sakuma Y, et al. Lab Invest. 2012, 92(3), 371-383. 3. Zannetti A, et al. J Nucl Med. 2012, 53(3), 443-450.

Related compound libraries

This product is contained In the following compound libraries:
Tyrosine Kinase Inhibitor Library Highly Selective Inhibitor Library Bioactive Compound Library Inhibitor Library Angiogenesis related Compound Library Anti-Lung Cancer Compound Library Kinase Inhibitor Library Cytokine Inhibitor Library JAK-STAT Compound Library Anti-Colorectal Cancer Compound Library

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Keywords

WZ4002 1213269-23-8 Angiogenesis JAK/STAT signaling Tyrosine Kinase/Adaptors EGFR WZ-4002 ErbB-1 inhibit Inhibitor Epidermal growth factor receptor HER1 WZ 4002 inhibitor

 

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