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WZ8040

Name: WZ8040
Brand: TargetMol
SKU: T6734
Price: 40 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T6734Cas No. 1214265-57-2

WZ8040 is a novel mutant-selective irreversible EGFRT790M inhibitor, does not inhibit ERBB2 phosphorylation (T798I).

WZ8040

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Purity: 99.78%

Catalog No. T6734Cas No. 1214265-57-2

WZ8040 is a novel mutant-selective irreversible EGFRT790M inhibitor, does not inhibit ERBB2 phosphorylation (T798I).

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$40	In Stock	In Stock
5 mg	$95	In Stock	In Stock
10 mg	$153	In Stock	In Stock
25 mg	$259	In Stock	In Stock
50 mg	$385	-	In Stock
100 mg	$567	-	In Stock
1 mL x 10 mM (in DMSO)	$97	In Stock	In Stock

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

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Purity:99.78%

Appearance:Solid

Color:White to Yellow

Resource Download

COA LCMS HNMR

Product Introduction

Bioactivity

Description	WZ8040 is a novel mutant-selective irreversible EGFRT790M inhibitor, does not inhibit ERBB2 phosphorylation (T798I).
Targets&IC50	EGFR/ERBB2 (wildtype):1.82 μM (in HN11 cells), HCC827 GR cells (EGFR E746_A750/MET amp):>3.3 μM, H1975 cells (EGFR L858R/T790M):9 nM, H1781 cells (ErbB2 Ins G776V, C):744 nM, Calu3 (ErbB2 amp):915 nM, PC9 cells (EGFR Del E746_A750):6 nM, H3255 cells (EGFR L858R):66 nM, PC9 GR cells (EGFR Del E746_A750/T790M):8 nM, HCC827 cells (EGFR Del E746_A750):1 nM, H1819 cells (ErbB2 amp):738 nM
In vitro	WZ8040 is 30- to 100-fold more potent against EGFR T790M, and up to 100-fold less potent against wild-type EGFR, than quinazoline-based EGFR inhibitors such as CL-387785 and HKI-272. WZ8040 treatment potently inhibits the growth of HCC827 (EGFR Del E746_A750), PC9 (EGFR Del E746_A750), H3255 (EGFR L858R), H1975 (EGFR L858R/T790M), and PC9 GR (EGFR Del E746_A750/T790M) with IC50 of 1 nM, 6 nM, 66 nM, 9 nM, and 8 nM, respectively. WZ8040 weakly inhibits the growth of HCC827 GR (EGFR E746_A750/MET amp), H1819 (ERBB2 amp), Calu-3 (ERBB2 amp), H1781 (ERBB2 Ins G776V, C), and HN11 (EGFR & ERBB2 WT) with IC50 of >3.3 μM, 738 nM, 915 nM, 744 nM, and 1.82 μM, respectively. WZ8040 is not toxic up to 10 μM against A549 (KRAS mutant) or H3122 (EML4-ALK) cells. [1]
Cell Research	Cells are exposed to increasing concentrations of WZ8040 for 72 hours. Growth is assessed using the MTS survival assay.(Only for Reference)

Chemical Properties

Molecular Weight	481.01
Formula	C₂₄H₂₅ClN₆OS
Cas No.	1214265-57-2
Smiles	CN1CCN(CC1)c1ccc(Nc2ncc(Cl)c(Sc3cccc(NC(=O)C=C)c3)n2)cc1
Relative Density.	1.37 g/cm3

Storage & Solubility Information

Storage

store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

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

Ethanol: 3 mg/mL (6.24 mM), Sonication is recommended.

DMSO: 89 mg/mL (185.03 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (4.16 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

Ethanol/DMSO

	1mg	5mg	10mg	50mg
1 mM	2.0790 mL	10.3948 mL	20.7896 mL	103.9479 mL
5 mM	0.4158 mL	2.0790 mL	4.1579 mL	20.7896 mL

DMSO

	1mg	5mg	10mg	50mg
10 mM	0.2079 mL	1.0395 mL	2.0790 mL	10.3948 mL
20 mM	0.1039 mL	0.5197 mL	1.0395 mL	5.1974 mL
50 mM	0.0416 mL	0.2079 mL	0.4158 mL	2.0790 mL
100 mM	0.0208 mL	0.1039 mL	0.2079 mL	1.0395 mL

Calculator

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc