Catalog No.S1173

WZ4002 Chemical Structure

Molecular Weight(MW): 494.18

WZ4002 is a novel, mutant-selective EGFR inhibitor for EGFR(L858R)/(T790M) with IC50 of 2 nM/8 nM in BaF3 cell line; does not inhibit ERBB2 phosphorylation (T798I).

Size Price Stock Quantity  
In DMSO USD 109 In stock
USD 120 In stock
USD 370 In stock
USD 670 In stock
Bulk Discount

Free Overnight Delivery on orders over $ 500
Next day delivery by 10:00 a.m. Order now.

Cited by 24 Publications

Purity & Quality Control

Choose Selective EGFR Inhibitors

Biological Activity

Description WZ4002 is a novel, mutant-selective EGFR inhibitor for EGFR(L858R)/(T790M) with IC50 of 2 nM/8 nM in BaF3 cell line; does not inhibit ERBB2 phosphorylation (T798I).
EGFR (L858R) [1]
(BaF3 cells)
EGFR (L858R/T790M) [1]
(BaF3 cells)
2 nM 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]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
Sf9 cells NXP5R2p6TnWwY4Tpc44h[XO|YYm= NXTBfVk{PjBibXnudy=> M2nqcWlvcGmkaYTpc44hd2ZiRVfGVkBNQDV6UjDteZRidnRiKIXub45wf25ib4Lp[4lvMSCneIDy[ZN{\WRiaX6gV4Y6KGOnbHzzJJBz\S2rbnP1ZoF1\WRiZn;yJFYxKG2rboOgZoVnd3KnIIP1ZpN1emG2ZTDhcoQhSVSSIHHk[Il1cW:wIHL5JIhwdW:pZX7lc5V{KHSrbXWtdoV{d2y4ZXSgSnJGXCCjc4PhfUwhUUN3ME2xJI5O Ml;rNlYzPzVyMki=
mouse BA/F3 cells NFLCcI5Rem:uaX\ldoF1cW:wIHHzd4F6 NIPXTYJCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JI1wfXOnIFLBM2Y{KGOnbHzzJJRz[W6|ZnXjeIVlKHerdHigSWdHWiCHN{S2Y2E4PTChZHXsM3Q4QTCPIH31eIFvfCxiRVO1NF0zKG6P MV2yNVIxQDhyMh?=
human HCC827 cells NYnVSmdFWHKxbHnm[ZJifGmxbjDhd5NigQ>? NVOwemRLPzJiaB?= M2\qPGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iSFPDPFI4KGOnbHzzJIhiemKxcnnu[{BGT0[UIHTlcEBGPzR4LVG3OVAhdXW2YX70JIFnfGW{IEeyJIhzeyCkeTDNWHMh[XO|YYmsJGlEPTB;NzDuUS=> NWPLdpRxOjJ|M{mzOFI>
human PC9 cells NIizeYpRem:uaX\ldoF1cW:wIHHzd4F6 M{PnXWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4Sg[5Jwf3SqLYLld4l{fGGwdDDoeY1idiCSQ{mgZ4VtdHNiZYjwdoV{e2mwZzDFS2ZTKEV5NE\fRVc2OC:WN{mwUUBufXSjboSsJGVEPTB;MUSgcm0> MnLRNlEzODh6MEK=
NCI-H1975 cells NVfONnFKTnWwY4Tpc44h[XO|YYm= NVzWT286OiCq M4XwfmlvcGmkaYTpc44hd2ZiRVfGVkBNQDV6Uj;UPVcxVSCmb4XicIUhdXW2YX70JJBpd3OyaH;yfYxifGmxbjDpckBpfW2jbjDOR2kuUDF7N{WgZ4VtdHNiYX\0[ZIhOiCqcoOgZpkh\my3b4Lld4NmdmOnIHHzd4F6NCCLQ{WwQVAvODJ|IN88US=> NGS2c3YzOzl|MEm5OC=>
human 16HBE cells Mo\wVJJwdGmoZYLheIlwdiCjc4PhfS=> NF7meYc4OiCq MVjBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKDF4SFLFJINmdGy|IHX4dJJme3Orbnege4lt\CC2eYDlJGVITlJiYX\0[ZIhPzJiaILzJIJ6KE2WVDDhd5NigSxiSVO1NF0xNjhzMTFOwG0> NGrFRYIzOzd7MkOxPC=>
human A431 cells NEfPSYxEgXSxdH;4bYNqfHliYYPzZZk> NXftXmxZPzJiaB?= NGf5cVZEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBCPDNzIHPlcIx{KG:4ZYLlfJBz\XO|aX7nJJdqdGRidInw[UBGT0[UIHHzd4V{e2WmIHHzJIdzd3e2aDDpcohq[mm2aX;uJIFnfGW{IEeyJIhzeyCkeTDNWHQh[XO|YYmsJGlEPTB;MT6xNFgh|ryP M2qxflI{PjZ6NESx
human LoVo cells MofaSpVv[3Srb36gZZN{[Xl? NVTBXGNZOiCq NV;qVHhKUW6qaXLpeIlwdiCxZjD3bYxlKHS7cHWgSWdHWiCyaH;zdIhwenmuYYTpc44hcW5iaIXtZY4hVG:YbzDj[YxteyCjZoTldkAzKGi{czDifUBndHWxcnXzZ4Vv[2ViYYPzZZktKEmFNUC9NU4yQCEQvF2= NVy1c|FiOjN7M{C5PVQ>
human 16HBE14o- cells  MWnDfZRwfG:6aXPpeJkh[XO|YYm= NFO4WFc4OiCq MYnDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjCxOmhDTTF2bz2gZ4VtdHNiaHHyZo9zcW6pIIfpcIQhfHmyZTDFS2ZTKGG|c3Xzd4VlKGG|IHfyc5d1cCCrbnjpZol1cW:wIHHmeIVzKDd{IHjyd{BjgSCPVGSgZZN{[XluIFnDOVA:OS5|NUWg{txO MoH3NlM3Pjh2NEG=
human BEAS2B cells NXq3UXJXS3m2b4TvfIlkcXS7IHHzd4F6 NEm1ZWg4OiCq MY\DfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDCSWFUOkJiY3XscJMhcGG{Yn;ybY5oKHerbHSgeJlx\SCHR1\SJIF{e2W|c3XkJIF{KGe{b4f0bEBqdmirYnn0bY9vKGGodHXyJFczKGi{czDifUBOXFRiYYPzZZktKEmFNUC9NU45OTFizszN M{fVZVI{PjZ6NESx
human A549 cells MnLMVJJwdGmoZYLheIlwdiCjc4PhfS=> M1HRdVczKGh? NHiyVHhCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIsuWkGVIHTldIVv\GWwdDDoeY1idiCDNUS5JINmdGy|IH;2[ZJmgHC{ZYPzbY5oKFeWIFXHSnIh[W[2ZYKgO|IhcHK|IHL5JG1VXCCjc4PhfUwhUUN3ME2yMlExOiEQvF2= MmTDNlQ3ODd3OUG=
human HL7702 cells MXrQdo9tcW[ncnH0bY9vKGG|c3H5 M3vScVczKGh? M4S2WmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iSFy3O|AzKGOnbHzzJIV5eHKnc4Ppcochf2mudDD0fZBmKEWJRmKgZYZ1\XJiN{KgbJJ{KGK7IF3UV{Bie3OjeTygTWM2OD1{LkezJO69VQ>? MV2yNlM{QTN2Mh?=

... Click to View More Cell Line Experimental Data

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:[1]
- Collapse

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:[1]
- Collapse
  • Cell lines: NSCLC, Ba/F3 cells, NIH-3T3 cells, PC9GR4 cells
  • Concentrations: 0-1 μM
  • Incubation Time: 72 hours
  • Method: The NSCLC, Ba/F3 cells, NIH-3T3 cells, PC9GR4 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)
Animal Research:[1]
- Collapse
  • Animal Models: EGFR-TL (T790M/L858R) mice
  • Formulation: NMP (10% 1-methyl-2-pyrrolidinone: 90% PEG-300
  • Dosages: 25mg/kg
  • Administration: Gavage
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 13 mg/mL (26.3 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
30% PEG400+0.5% Tween80+5% propylene glycol
For best results, use promptly after mixing.
30 mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 494.18


CAS No. 1213269-23-8
Storage powder
in solvent
Synonyms N/A

Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

  • Mass
    Molecular Weight

*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

  • C1

* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

  • Serial Dilutions

  • Computed Result

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

  • * Indicates a Required Field

EGFR Signaling Pathway Map

EGFR Inhibitors with Unique Features

Related EGFR Products

Tags: buy WZ4002 | WZ4002 supplier | purchase WZ4002 | WZ4002 cost | WZ4002 manufacturer | order WZ4002 | WZ4002 distributor
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID