WZ4002

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).
Targets
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 MoSzSpVv[3Srb36gZZN{[Xl? M17vXlYxKG2rboO= MVPJcohq[mm2aX;uJI9nKEWJRmKgUFg2QFJibYX0ZY51KCi3bnvuc5dvKG:{aXfpckkh\XiycnXzd4VlKGmwIGPmPUBk\WyuczDwdoUucW6ldXLheIVlKG[xcjC2NEBucW6|IHLl[o9z\SC|dXLzeJJifGViYX7kJGFVWCCjZHTpeIlwdiCkeTDoc41w\2WwZX;1d{B1cW2nLYLld49tfmWmIF\SSXQh[XO|YYmsJGlEPTB;MTDuUS=> NVLPcmp5OjZ{N{WwNlg>
mouse BA/F3 cells NFf4NlFRem:uaX\ldoF1cW:wIHHzd4F6 NX3zc486SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBud3W|ZTDCRU9HOyClZXzsd{B1emGwc3\lZ5Rm\CC5aYToJGVITlJiRUe0On9CPzVyX3TlcE9VPzlyTTDteZRidnRuIFXDOVA:OiCwTR?= M{TldVIyOjB6OECy
human HCC827 cells MofJVJJwdGmoZYLheIlwdiCjc4PhfS=> M2rVTlczKGh? M{LSVWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iSFPDPFI4KGOnbHzzJIhiemKxcnnu[{BGT0[UIHTlcEBGPzR4LVG3OVAhdXW2YX70JIFnfGW{IEeyJIhzeyCkeTDNWHMh[XO|YYmsJGlEPTB;NzDuUS=> NFfTPHgzOjN|OUO0Ni=>
human PC9 cells M1zXXnBzd2yrZnXyZZRqd25iYYPzZZk> NXmyU49RSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBoem:5dHitdoV{cXO2YX70JIh2dWGwIGDDPUBk\WyuczDlfJBz\XO|aX7nJGVITlJiRUe0On9CPzVyL2S3PVBOKG23dHHueEwhTUN3ME2xOEBvVQ>? MnG3NlEzODh6MEK=
NCI-H1975 cells NEnxblNHfW6ldHnvckBie3OjeR?= NEf5WVYzKGh? M3KwXWlvcGmkaYTpc44hd2ZiRVfGVkBNQDV6Uj;UPVcxVSCmb4XicIUhdXW2YX70JJBpd3OyaH;yfYxifGmxbjDpckBpfW2jbjDOR2kuUDF7N{WgZ4VtdHNiYX\0[ZIhOiCqcoOgZpkh\my3b4Lld4NmdmOnIHHzd4F6NCCLQ{WwQVAvODJ|IN88US=> MWeyN|k{ODl7NB?=
human 16HBE cells NGO0[oFRem:uaX\ldoF1cW:wIHHzd4F6 NXLuVZN1PzJiaB?= MlzBRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiBzNljCSUBk\WyuczDlfJBz\XO|aX7nJJdqdGRidInw[UBGT0[UIHHmeIVzKDd{IHjyd{BjgSCPVGSgZZN{[XluIFnDOVA:OC56MUGg{txO NUjGSJBqOjN5OUKzNVg>
human A431 cells MlPvR5l1d3SxeHnjbZR6KGG|c3H5 NYf6O4xVPzJiaB?= M1PCZWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGE1OzFiY3XscJMhd3[ncnX4dJJme3Orbnege4lt\CC2eYDlJGVITlJiYYPz[ZN{\WRiYYOg[5Jwf3SqIHnubIljcXSrb36gZYZ1\XJiN{KgbJJ{KGK7IF3UWEBie3OjeTygTWM2OD1zLkGwPEDPxE1? Mlq1NlM3Pjh2NEG=
human LoVo cells MoTmSpVv[3Srb36gZZN{[Xl? MUWyJIg> NHXzdolKdmirYnn0bY9vKG:oIIfpcIQhfHmyZTDFS2ZTKHCqb4PwbI9zgWyjdHnvckBqdiCqdX3hckBNd1[xIHPlcIx{KGGodHXyJFIhcHK|IHL5JIZtfW:{ZYPj[Y5k\SCjc4PhfUwhUUN3ME2xMlE5KM7:TR?= Mm\ENlM6OzB7OUS=
human 16HBE14o- cells  M4TROGN6fG:2b4jpZ4l1gSCjc4PhfS=> MYC3NkBp NFjReYZEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckAyPkiERUG0c{0h[2WubIOgbIFz[m:{aX7nJJdqdGRidInw[UBGT0[UIHHzd4V{e2WmIHHzJIdzd3e2aDDpcohq[mm2aX;uJIFnfGW{IEeyJIhzeyCkeTDNWHQh[XO|YYmsJGlEPTB;MT6zOVUh|ryP NYLFVlVlOjN4Nki0OFE>
human BEAS2B cells M4jhSWN6fG:2b4jpZ4l1gSCjc4PhfS=> NXrtWYE{PzJiaB?= M4TuUmN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGJGSVN{QjDj[YxteyCqYYLic5Jqdmdid3ns[EB1gXCnIFXHSnIh[XO|ZYPz[YQh[XNiZ4Lve5RpKGmwaHnibZRqd25iYX\0[ZIhPzJiaILzJIJ6KE2WVDDhd5NigSxiSVO1NF0yNjhzMTFOwG0> NYjnNHA{OjN4Nki0OFE>
human A549 cells M1G2S3Bzd2yrZnXyZZRqd25iYYPzZZk> MnOwO|IhcA>? MWXBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHutVmFUKGSncHXu[IVvfCCqdX3hckBCPTR7IHPlcIx{KG:4ZYLlfJBz\XO|aX7nJHdVKEWJRmKgZYZ1\XJiN{KgbJJ{KGK7IF3UWEBie3OjeTygTWM2OD1{LkGwNkDPxE1? MnjMNlQ3ODd3OUG=
human HL7702 cells M1jMNnBzd2yrZnXyZZRqd25iYYPzZZk> M17BOVczKGh? M{PNWmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iSFy3O|AzKGOnbHzzJIV5eHKnc4Ppcochf2mudDD0fZBmKEWJRmKgZYZ1\XJiN{KgbJJ{KGK7IF3UV{Bie3OjeTygTWM2OD1{LkezJO69VQ>? MojDNlI{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]

Protocol

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 individually and in order:
30% PEG400+0.5% Tween80+5% propylene glycol
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
Formula

C25H27ClN6O3

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

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID