For research use only.

Catalog No.S1173

34 publications

WZ4002 Chemical Structure

CAS No. 1213269-23-8

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).

Selleck's WZ4002 has been cited by 34 publications

Purity & Quality Control

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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 NHnKWo5HfW6ldHnvckBie3OjeR?= NFm2XlI3OCCvaX7z NFqwVWlKdmirYnn0bY9vKG:oIFXHSnIhVDh3OGKgcZV1[W62IDj1cotvd3ewIH;ybYdqdiliZYjwdoV{e2WmIHnuJHNnQSClZXzsd{BxemVvaX7jeYJifGWmIH\vdkA3OCCvaX7zJIJm\m:{ZTDzeYJ{fHKjdHWgZY5lKEGWUDDh[IRqfGmxbjDifUBpd22xZ3Xu[Y92eyC2aX3lMZJme2:udnXkJGZTTVRiYYPzZZktKEmFNUC9NUBvVQ>? NGnnfGgzPjJ5NUCyPC=>
mouse BA/F3 cells M2m2c3Bzd2yrZnXyZZRqd25iYYPzZZk> NGDCR2dCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JI1wfXOnIFLBM2Y{KGOnbHzzJJRz[W6|ZnXjeIVlKHerdHigSWdHWiCHN{S2Y2E4PTChZHXsM3Q4QTCPIH31eIFvfCxiRVO1NF0zKG6P MYKyNVIxQDhyMh?=
human HCC827 cells NVPobY9wWHKxbHnm[ZJifGmxbjDhd5NigQ>? MVq3NkBp MV3BcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEiFQ{iyO{Bk\WyuczDoZZJjd3KrbnegSWdHWiCmZXygSVc1Pi2DN{WwJI12fGGwdDDh[pRmeiB5MjDodpMh[nliTWTTJIF{e2G7LDDJR|UxRTdibl2= NFHX[WgzOjN|OUO0Ni=>
human PC9 cells NV30U5hSWHKxbHnm[ZJifGmxbjDhd5NigQ>? NYHxeplISW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBoem:5dHitdoV{cXO2YX70JIh2dWGwIGDDPUBk\WyuczDlfJBz\XO|aX7nJGVITlJiRUe0On9CPzVyL2S3PVBOKG23dHHueEwhTUN3ME2xOEBvVQ>? NIX6N2IzOTJyOEiwNi=>
NCI-H1975 cells M1P3fGZ2dmO2aX;uJIF{e2G7 NVTERmp3OiCq MWXJcohq[mm2aX;uJI9nKEWJRmKgUFg2QFJxVEm3NG0h\G:3YnzlJI12fGGwdDDwbI9{eGixconsZZRqd25iaX6gbJVu[W5iTlPJMWgyQTd3IHPlcIx{KGGodHXyJFIhcHK|IHL5JIZtfW:{ZYPj[Y5k\SCjc4PhfUwhUUN3ME2wMlAzOyEQvF2= NVm2fWNkOjN7M{C5PVQ>
human 16HBE cells NVXDeI1UWHKxbHnm[ZJifGmxbjDhd5NigQ>? M1r5e|czKGh? M3fuU2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iMU\IRmUh[2WubIOg[ZhxemW|c3nu[{B4cWymIIT5dIUhTUeIUjDh[pRmeiB5MjDodpMh[nliTWTUJIF{e2G7LDDJR|UxRTBwOEGxJO69VQ>? M3HDUVI{Pzl{M{G4
human A431 cells M4HZeGN6fG:2b4jpZ4l1gSCjc4PhfS=> MWS3NkBp NEXybohEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBCPDNzIHPlcIx{KG:4ZYLlfJBz\XO|aX7nJJdqdGRidInw[UBGT0[UIHHzd4V{e2WmIHHzJIdzd3e2aDDpcohq[mm2aX;uJIFnfGW{IEeyJIhzeyCkeTDNWHQh[XO|YYmsJGlEPTB;MT6xNFgh|ryP MXeyN|Y3QDR2MR?=
human LoVo cells Mn7USpVv[3Srb36gZZN{[Xl? MoLQNkBp NEf2d|hKdmirYnn0bY9vKG:oIIfpcIQhfHmyZTDFS2ZTKHCqb4PwbI9zgWyjdHnvckBqdiCqdX3hckBNd1[xIHPlcIx{KGGodHXyJFIhcHK|IHL5JIZtfW:{ZYPj[Y5k\SCjc4PhfUwhUUN3ME2xMlE5KM7:TR?= MVuyN|k{ODl7NB?=
human 16HBE14o- cells  MYHDfZRwfG:6aXPpeJkh[XO|YYm= NGXJNmY4OiCq NUjwSVJzS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hOT[KQlWxOI8uKGOnbHzzJIhiemKxcnnu[{B4cWymIIT5dIUhTUeIUjDhd5Nme3OnZDDhd{Boem:5dHigbY5pcWKrdHnvckBi\nSncjC3NkBpenNiYomgUXRVKGG|c3H5MEBKSzVyPUGuN|U2KM7:TR?= MWKyN|Y3QDR2MR?=
human BEAS2B cells M2TFTGN6fG:2b4jpZ4l1gSCjc4PhfS=> MlX1O|IhcA>? M{XxbmN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGJGSVN{QjDj[YxteyCqYYLic5Jqdmdid3ns[EB1gXCnIFXHSnIh[XO|ZYPz[YQh[XNiZ4Lve5RpKGmwaHnibZRqd25iYX\0[ZIhPzJiaILzJIJ6KE2WVDDhd5NigSxiSVO1NF0yNjhzMTFOwG0> Mn;wNlM3Pjh2NEG=
human A549 cells NHjtVlFRem:uaX\ldoF1cW:wIHHzd4F6 MX63NkBp M{DIXWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4Sgb{1TSVNiZHXw[Y5l\W62IHj1cYFvKEF3NEmgZ4VtdHNib4\ldoV5eHKnc4PpcochX1RiRVfGVkBi\nSncjC3NkBpenNiYomgUXRVKGG|c3H5MEBKSzVyPUKuNVAzKM7:TR?= M4PofFI1PjB5NUmx
human HL7702 cells MUjQdo9tcW[ncnH0bY9vKGG|c3H5 NXPmVXUxPzJiaB?= MVLBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEiON{ewNkBk\WyuczDlfJBz\XO|aX7nJJdqdHRidInw[UBGT0[UIHHmeIVzKDd{IHjyd{BjgSCPVGOgZZN{[XluIFnDOVA:Oi55MzFOwG0> NUjzOIZJOjJ|M{mzOFI>

... 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]
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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]
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  • 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]
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  • Animal Models: EGFR-TL (T790M/L858R) mice
  • 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
Smiles CN1CCN(CC1)C2=CC(=C(C=C2)NC3=NC=C(C(=N3)OC4=CC=CC(=C4)NC(=O)C=C)Cl)OC

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID