WZ4002

For research use only.

Catalog No.S1173

29 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).

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10mM (1mL in DMSO) RMB 891.25 In stock
RMB 983.91 In stock
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Selleck's WZ4002 has been cited by 29 publications

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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).
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 Ml;MSpVv[3Srb36gZZN{[Xl? NYHiUoZjPjBibXnudy=> NFfRbmZKdmirYnn0bY9vKG:oIFXHSnIhVDh3OGKgcZV1[W62IDj1cotvd3ewIH;ybYdqdiliZYjwdoV{e2WmIHnuJHNnQSClZXzsd{BxemVvaX7jeYJifGWmIH\vdkA3OCCvaX7zJIJm\m:{ZTDzeYJ{fHKjdHWgZY5lKEGWUDDh[IRqfGmxbjDifUBpd22xZ3Xu[Y92eyC2aX3lMZJme2:udnXkJGZTTVRiYYPzZZktKEmFNUC9NUBvVQ>? MYSyOlI4PTB{OB?=
mouse BA/F3 cells NIDiNoJRem:uaX\ldoF1cW:wIHHzd4F6 NEW3cndCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JI1wfXOnIFLBM2Y{KGOnbHzzJJRz[W6|ZnXjeIVlKHerdHigSWdHWiCHN{S2Y2E4PTChZHXsM3Q4QTCPIH31eIFvfCxiRVO1NF0zKG6P MWKyNVIxQDhyMh?=
human HCC827 cells M2LSV3Bzd2yrZnXyZZRqd25iYYPzZZk> MojFO|IhcA>? M4DiWmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iSFPDPFI4KGOnbHzzJIhiemKxcnnu[{BGT0[UIHTlcEBGPzR4LVG3OVAhdXW2YX70JIFnfGW{IEeyJIhzeyCkeTDNWHMh[XO|YYmsJGlEPTB;NzDuUS=> NGLtPVgzOjN|OUO0Ni=>
human PC9 cells MmnDVJJwdGmoZYLheIlwdiCjc4PhfS=> M3Gz[mFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4Sg[5Jwf3SqLYLld4l{fGGwdDDoeY1idiCSQ{mgZ4VtdHNiZYjwdoV{e2mwZzDFS2ZTKEV5NE\fRVc2OC:WN{mwUUBufXSjboSsJGVEPTB;MUSgcm0> M2L1bFIyOjB6OECy
NCI-H1975 cells NVrMT4V1TnWwY4Tpc44h[XO|YYm= MkSwNkBp MmPwTY5pcWKrdHnvckBw\iCHR1\SJGw5PTiUL2S5O|BOKGSxdXLs[UBufXSjboSgdIhwe3Cqb4L5cIF1cW:wIHnuJIh2dWGwIF7DTU1JOTl5NTDj[YxteyCjZoTldkAzKGi{czDifUBndHWxcnXzZ4Vv[2ViYYPzZZktKEmFNUC9NE4xOjNizszN MVWyN|k{ODl7NB?=
human 16HBE cells MXvQdo9tcW[ncnH0bY9vKGG|c3H5 MWC3NkBp M4nzd2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iMU\IRmUh[2WubIOg[ZhxemW|c3nu[{B4cWymIIT5dIUhTUeIUjDh[pRmeiB5MjDodpMh[nliTWTUJIF{e2G7LDDJR|UxRTBwOEGxJO69VQ>? NEfKWo4zOzd7MkOxPC=>
human A431 cells MULDfZRwfG:6aXPpeJkh[XO|YYm= MX:3NkBp NX\FT|BCS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hSTR|MTDj[YxteyCxdnXy[ZhxemW|c3nu[{B4cWymIIT5dIUhTUeIUjDhd5Nme3OnZDDhd{Boem:5dHigbY5pcWKrdHnvckBi\nSncjC3NkBpenNiYomgUXRVKGG|c3H5MEBKSzVyPUGuNVA5KM7:TR?= MlvXNlM3Pjh2NEG=
human LoVo cells MnTvSpVv[3Srb36gZZN{[Xl? NUG0RohYOiCq M1rXeWlvcGmkaYTpc44hd2Zid3ns[EB1gXCnIFXHSnIheGixc4Doc5J6dGG2aX;uJIlvKGi3bXHuJGxwXm9iY3XscJMh[W[2ZYKgNkBpenNiYomg[ox2d3Knc3PlcoNmKGG|c3H5MEBKSzVyPUGuNVgh|ryP NFTPfJozOzl|MEm5OC=>
human 16HBE14o- cells  MmXjR5l1d3SxeHnjbZR6KGG|c3H5 M{fTeVczKGh? NWLNbWp[S3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hOT[KQlWxOI8uKGOnbHzzJIhiemKxcnnu[{B4cWymIIT5dIUhTUeIUjDhd5Nme3OnZDDhd{Boem:5dHigbY5pcWKrdHnvckBi\nSncjC3NkBpenNiYomgUXRVKGG|c3H5MEBKSzVyPUGuN|U2KM7:TR?= MVWyN|Y3QDR2MR?=
human BEAS2B cells MV;DfZRwfG:6aXPpeJkh[XO|YYm= M1;RRlczKGh? NV\uNVM6S3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hSkWDU{LCJINmdGy|IHjhdoJwemmwZzD3bYxlKHS7cHWgSWdHWiCjc4Pld5Nm\CCjczDndo94fGhiaX7obYJqfGmxbjDh[pRmeiB5MjDodpMh[nliTWTUJIF{e2G7LDDJR|UxRTFwOEGxJO69VQ>? MUiyN|Y3QDR2MR?=
human A549 cells NFLvVItRem:uaX\ldoF1cW:wIHHzd4F6 MYm3NkBp M37yS2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4Sgb{1TSVNiZHXw[Y5l\W62IHj1cYFvKEF3NEmgZ4VtdHNib4\ldoV5eHKnc4PpcochX1RiRVfGVkBi\nSncjC3NkBpenNiYomgUXRVKGG|c3H5MEBKSzVyPUKuNVAzKM7:TR?= NX3weFlXOjR4MEe1PVE>
human HL7702 cells NXjldWNNWHKxbHnm[ZJifGmxbjDhd5NigQ>? Mne4O|IhcA>? NI\OWGlCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFjMO|cxOiClZXzsd{BmgHC{ZYPzbY5oKHerbISgeJlx\SCHR1\SJIFnfGW{IEeyJIhzeyCkeTDNWHMh[XO|YYmsJGlEPTB;Mj63N{DPxE1? MVqyNlM{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]

Protocol

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
Formula

C25H27ClN6O3

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