WZ4002

Cat. No.: HY-12026 Purity: 99.76%: FAQs
Data Sheet SDS COA Handling Instructions

WZ4002 is a mutant selective EGFR inhibitor with IC₅₀s of 2, 8, 3 and 2 nM for EGFR^L858R, EGFR^L858R/T790M, EGFR^E746_A750 and EGFR^{E746_A750/T790M}, respectively.

For research use only. We do not sell to patients.

WZ4002 Chemical Structure

CAS No. : 1213269-23-8

Size	Price	Stock	Quantity

Free Sample (0.1 - 0.5 mg)		Apply Now
Solution
10 mM * 1 mL in DMSO	USD 92	In-stock	Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL ready for reconstitution	USD 92	In-stock	Estimated Time of Arrival: December 31
Solid
10 mg	USD 84	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 240	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 420	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 9 publication(s) in Google Scholar

6 Publications Citing Use of MCE WZ4002

: WZ4002 purchased from MCE. Usage Cited in: Oncotarget. 2016 Oct 25;7(43):69760-69769. [Abstract]; Ibrutinib and WZ4002 inhibitory effects on EGFRY1068 auto-phosphorylation in the H1975 cell line at different time points by removal of drug after 4 h pretreatment

: WZ4002 purchased from MCE. Usage Cited in: Oncotarget. 2015 Oct 13;6(31):31313-22. [Abstract]; Effect of Ibrutinib on EGFR wt/mutant NSCLCs. Ibrutinib effects on wt EGFR and mutant EGFR- mediated signaling pathways. The results demonstrate that Ibrutinib potently inhibits both EGFR wt/mutant auto-phosphorylation at Y1068.

: WZ4002 purchased from MCE. Usage Cited in: Oncotarget. 2015 Oct 13;6(31):31313-22. [Abstract]; Effect of Ibrutinib, WZ4002, AZD9291 and CO1686 on EGFR phosphorylation of tyrosines 1068 and 1173 in EGFR-dependent cancer cell lines.

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EGFR/ErbB1/HER1 ErbB2/HER2 ErbB3/HER3 ErbB4/HER4

Biological Activity
Protocol
Purity & Documentation
References
Customer Review

Description

WZ4002 is a mutant selective EGFR inhibitor with IC₅₀s of 2, 8, 3 and 2 nM for EGFR^L858R, EGFR^L858R/T790M, EGFR^E746_A750 and EGFR^{E746_A750/T790M}, respectively.

IC₅₀ & Target^[1]

EGFR^L858R

2 nM (IC₅₀, Cell Assay)

EGFR^L858R/T790M

8 nM (IC₅₀, Cell Assay)

EGFR^E746_A750

3 nM (IC₅₀, Cell Assay)

EGFR^{E746_A750/T790M}

2 nM (IC₅₀, Cell Assay)

In Vitro

WZ4002 increases cellular potency correlated with inhibition of EGFR, AKT and ERK1/2 phosphorylation in NSCLC cell lines and EGFR phosphorylation in NIH-3T3 cells expressing different EGFR^T790M mutant alleles. WZ4002 inhibits EGFR kinase activity of recombinant L858R/T790M protein more potently than of WT EGFR^[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

In a pharmacodynamic study WZ4002 effectively inhibits EGFR, AKT and ERK1/2 phosphorylation which is associated with a significant increase in TUNEL positive and a significant decrease in Ki67 positive cells compared to vehicle alone treated mice. In a 2 week efficacy study, WZ4002 treatment results in significant tumor regressions compared to vehicle alone in both T790M containing murine models. Histological evaluation of the lungs following treatment confirms significant resolution of the tumor nodules with only few small residual nodules and nodule remnants that has evidence of treatment effect with decreased cellularity and increased fibrosis consistent with remodeling/scarring^[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

494.97

Appearance

Solid

Formula

C₂₅H₂₇ClN₆O₃

CAS No.

1213269-23-8

SMILES

COC1=C(C=CC(N2CCN(CC2)C)=C1)NC3=NC=C(C(OC4=CC(NC(C=C)=O)=CC=C4)=N3)Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvent & Solubility

In Vitro:

DMSO : 10 mg/mL (20.20 mM; Need ultrasonic)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.0203 mL	10.1016 mL	20.2032 mL
5 mM	0.4041 mL	2.0203 mL	4.0406 mL
10 mM	0.2020 mL	1.0102 mL	2.0203 mL

*Please refer to the solubility information to select the appropriate solvent.

Purity & Documentation

Purity: 99.76%

Select Batch:

Data Sheet (273 KB) SDS (393 KB)

COA (244 KB) LCMS (270 KB)

Handling Instructions (2659 KB)

References

[1]. Zhou W, et al. Novel mutant-selective EGFR kinase inhibitors against EGFR T790M.Nature. 2009 Dec 24;462(7276):1070-4. [Content Brief]

Kinase Assay ^[1]	EGFR kinase assay is performed using a GST-kinase fusion protein. The final reaction mixture contained 60 mM HEPES pH 7.5, 5 mM MgCl₂, 5 mM MnCl₂, 3 mM Na₃V0₄, 1.25 mM DTT, 20 μM ATP, 1.5 μM PTP1B (Tyr66) biotinylated peptide and 50 ng of EGFR kinase. A phospotyrosine mab (pTyr100) is used to detect phosphorylation of the EGFR substrate peptide in the presence of WZ4002, gefitinib or HKI-272 (concentration ranges 0-10 μM for all drugs) followed a fluorescent Anti-mouse IgG secondary antibody. Fluorescence emission is detected at 615 nm^[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Assay ^[1]	Growth and inhibition of growth is assessed by MTS assay. Ba/F3 cells are exposed to WZ4002 treatment for 72 hours. Growth and inhibition of growth is assessed by MTS assay^[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[1]	Cohorts of EGFR TL/CCSP-rtTA and EGFR TD/CCSP-rtTA are put on doxycycline diet at 5 weeks of age to induce the expression of mutant EGFR. These mice undergo MRI after 6 to 8 weeks of doxycycline diet to document and quantify the lung cancer burden before being assigned to various treatment study cohorts. There is a minimum of 3 mice per treatment group. Mice are then treated either with vehicle (NMP 13 (10% 1-methyl-2-pyrrolidinone: 90% PEG-300) alone or WZ4002 at 25mg/kg gavage daily. After 2 weeks of treatment, these mice undergo a second round of MRI to document their response to the treatment. MRIs and tumor burden measurement are performed^[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References	[1]. Zhou W, et al. Novel mutant-selective EGFR kinase inhibitors against EGFR T790M.Nature. 2009 Dec 24;462(7276):1070-4. [Content Brief]

WZ4002 Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Keywords:

WZ40021213269-23-8WZ 4002WZ-4002EGFREpidermal growth factor receptorErbB-1HER1Inhibitorinhibitorinhibit

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WZ4002

Customer Review

WZ4002 Related Antibodies

6 Publications Citing Use of MCE WZ4002

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•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All EGFR Isoform Specific Products:

Biological Activity

Protocol

Purity & Documentation

References

Customer Review

WZ4002 Related Antibodies

WZ4002 Related Classifications

Molarity Calculator

Dilution Calculator

The molarity calculator equation

The dilution calculator equation

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