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
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5 Customer Reviews

  • Antitum o r activity of WZ4002 and/or E7050 in mouse xenograft models of human tumors. SCID mice-bearing PC-9/Vec (A), PC-9/HGF#5 (B), H1975 (C), or HCC827ER (D) tumors were administered 25 mg/kg WZ4002 and/or E7050 once daily for 14 to 21 days. Tumor volume was measured using calipers on the indicated days. Mean?SE tumor volumes are shown for groups of 4 to 5 mice.

    Mol Cancer Ther 2012 11, 2149-57. WZ4002 purchased from Selleck.

    (A) Cells were treated with or without the indicated doses of WZ4002 for 5 h. EGFR-related signal molecules were assessed using Western blot analysis.

    Oncotarget, 2016, 7(16):22005-15. WZ4002 purchased from Selleck.

  • (a) Western blots examine the effects of WZ4002 alone or a combination of WZ4002 and ABT-263 in H1975 parental or SR cells in suspension. Cells were grown for 48 h and then treated with the indicated pharmacological agent(s) for another 24 h. The cleaved/total poly (ADP-ribose) polymerase-1 (PARP-1) ratio determined for each cell line using Image J software is also represented. The values are the means of three independent experiments. (b) Quantification of apoptotic cells assessed by PARP-1 cleavage from each cell line.

    Lab Invest 2011 92, 371-383. WZ4002 purchased from Selleck.

    Caspase 3/7 activation in H1975 SR cells and HCC827 cells. Cells were seeded and left in suspension for 24 h, and then untreated or treated with the indicated drug(s) for another 24 h before being assessed. Caspase activity was evaluated by using the Caspase-Glo 3/7 assay and normalized to a 1.0 arbitrary unit for the mean of three untreated wells.

    Lab Invest 2011 92, 371-383. WZ4002 purchased from Selleck.

  • For MTT assays, cells (2,000 ~ 5,000 cells/well) were subcultured into 96-well plates according to their growth properties. Cell proliferation was assayed at 72 hr after treatment of WZ4002 by adding 20 μl of 5 mg/ml 3-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) solution per 100 μl of growth medium. After incubating for 3-4 h at 37°C, the media were removed and 150 µl/well of MTT solvent (either absolute DMSO or isopropanol containing 4 mM HCl and 0.1% Nonidet-40) was added to dissolve the formazan.

    Dr. Yong-Weon Yi from Georgetown University Medical Center. WZ4002 purchased from Selleck.

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 NVK4XngzTnWwY4Tpc44h[XO|YYm= NWXhV3l6PjBibXnudy=> NX70[WZyUW6qaXLpeIlwdiCxZjDFS2ZTKEx6NUjSJI12fGGwdDCoeY5sdm:5bjDvdolocW5rIHX4dJJme3OnZDDpckBU\jliY3XscJMheHKnLXnuZ5Vj[XSnZDDmc5IhPjBibXnud{Bj\W[xcnWgd5Vje3S{YYTlJIFv\CCDVGCgZYRlcXSrb36gZpkhcG:vb3flcoVwfXNidHnt[U1z\XOxbI\l[EBHWkWWIHHzd4F6NCCLQ{WwQVEhdk1? NHLCT3gzPjJ5NUCyPC=>
mouse BA/F3 cells MomzVJJwdGmoZYLheIlwdiCjc4PhfS=> NEm5NIdCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JI1wfXOnIFLBM2Y{KGOnbHzzJJRz[W6|ZnXjeIVlKHerdHigSWdHWiCHN{S2Y2E4PTChZHXsM3Q4QTCPIH31eIFvfCxiRVO1NF0zKG6P MXWyNVIxQDhyMh?=
human HCC827 cells Mn3PVJJwdGmoZYLheIlwdiCjc4PhfS=> Mo[xO|IhcA>? NYXSS5dMSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDIR2M5OjdiY3XscJMhcGG{Yn;ybY5oKEWJRmKg[IVtKEV5NE[tRVc2OCCvdYThcpQh[W[2ZYKgO|IhcHK|IHL5JG1VWyCjc4PhfUwhUUN3ME23JI5O M32zXFIzOzN7M{Sy
human PC9 cells M3WxU3Bzd2yrZnXyZZRqd25iYYPzZZk> NIK4NYJCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIdzd3e2aD3y[ZNqe3SjboSgbJVu[W5iUFO5JINmdGy|IHX4dJJme3OrbnegSWdHWiCHN{S2Y2E4PTBxVEe5NG0hdXW2YX70MEBGSzVyPUG0JI5O NGrWRlUzOTJyOEiwNi=>
NCI-H1975 cells MlS1SpVv[3Srb36gZZN{[Xl? MUOyJIg> NFfRUYRKdmirYnn0bY9vKG:oIFXHSnIhVDh3OGKvWFk4OE1iZH;1ZoxmKG23dHHueEBxcG:|cHjvdplt[XSrb36gbY4hcHWvYX6gUmNKNUhzOUe1JINmdGy|IHHmeIVzKDJiaILzJIJ6KG[udX;y[ZNk\W6lZTDhd5NigSxiSVO1NF0xNjB{MzFOwG0> MljwNlM6OzB7OUS=
human 16HBE cells MmPHVJJwdGmoZYLheIlwdiCjc4PhfS=> MWK3NkBp NHTQfVhCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIEG2TGJGKGOnbHzzJIV5eHKnc4Ppcochf2muZDD0fZBmKEWJRmKgZYZ1\XJiN{KgbJJ{KGK7IF3UWEBie3OjeTygTWM2OD1yLkixNUDPxE1? MnnwNlM4QTJ|MUi=
human A431 cells MlHGR5l1d3SxeHnjbZR6KGG|c3H5 Mme0O|IhcA>? Mm\NR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gRVQ{OSClZXzsd{BwfmW{ZYjwdoV{e2mwZzD3bYxlKHS7cHWgSWdHWiCjc4Pld5Nm\CCjczDndo94fGhiaX7obYJqfGmxbjDh[pRmeiB5MjDodpMh[nliTWTUJIF{e2G7LDDJR|UxRTFwMUC4JO69VQ>? M2W1XlI{PjZ6NESx
human LoVo cells MULGeY5kfGmxbjDhd5NigQ>? MnTENkBp M3fJVWlvcGmkaYTpc44hd2Zid3ns[EB1gXCnIFXHSnIheGixc4Doc5J6dGG2aX;uJIlvKGi3bXHuJGxwXm9iY3XscJMh[W[2ZYKgNkBpenNiYomg[ox2d3Knc3PlcoNmKGG|c3H5MEBKSzVyPUGuNVgh|ryP Mn;xNlM6OzB7OUS=
human 16HBE14o- cells  NGXEb3BEgXSxdH;4bYNqfHliYYPzZZk> MkTVO|IhcA>? NVzxSoJES3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hOT[KQlWxOI8uKGOnbHzzJIhiemKxcnnu[{B4cWymIIT5dIUhTUeIUjDhd5Nme3OnZDDhd{Boem:5dHigbY5pcWKrdHnvckBi\nSncjC3NkBpenNiYomgUXRVKGG|c3H5MEBKSzVyPUGuN|U2KM7:TR?= MXeyN|Y3QDR2MR?=
human BEAS2B cells MlHXR5l1d3SxeHnjbZR6KGG|c3H5 Ml\oO|IhcA>? M2D4[2N6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGJGSVN{QjDj[YxteyCqYYLic5Jqdmdid3ns[EB1gXCnIFXHSnIh[XO|ZYPz[YQh[XNiZ4Lve5RpKGmwaHnibZRqd25iYX\0[ZIhPzJiaILzJIJ6KE2WVDDhd5NigSxiSVO1NF0yNjhzMTFOwG0> NYW4TY9xOjN4Nki0OFE>
human A549 cells NVzrOI1UWHKxbHnm[ZJifGmxbjDhd5NigQ>? MV63NkBp MoLWRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDrMXJCWyCmZYDlcoRmdnRiaIXtZY4hSTV2OTDj[YxteyCxdnXy[ZhxemW|c3nu[{BYXCCHR1\SJIFnfGW{IEeyJIhzeyCkeTDNWHQh[XO|YYmsJGlEPTB;Mj6xNFIh|ryP MmCxNlQ3ODd3OUG=
human HL7702 cells NVzxWmtbWHKxbHnm[ZJifGmxbjDhd5NigQ>? MXy3NkBp NGPQcGNCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFjMO|cxOiClZXzsd{BmgHC{ZYPzbY5oKHerbISgeJlx\SCHR1\SJIFnfGW{IEeyJIhzeyCkeTDNWHMh[XO|YYmsJGlEPTB;Mj63N{DPxE1? MnjmNlI{Ozl|NEK=

... 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]
+ Expand

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]
+ Expand
  • 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]
+ Expand
  • 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

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID