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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  • 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.




製品説明 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

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 Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
Sf9 cells NETrPVlHfW6ldHnvckBie3OjeR?= M2XuWlYxKG2rboO= MmTYTY5pcWKrdHnvckBw\iCHR1\SJGw5PTiUIH31eIFvfCBqdX7rco94diCxcnnnbY4qKGW6cILld5Nm\CCrbjDT[lkh[2WubIOgdJJmNWmwY4XiZZRm\CCob4KgOlAhdWmwczDi[YZwemVic4Xid5Rz[XSnIHHu[EBCXFBiYXTkbZRqd25iYomgbI9ud2enbnXveZMhfGmvZT3y[ZNwdH[nZDDGVmVVKGG|c3H5MEBKSzVyPUGgcm0> M{n3UFI3Ojd3MEK4
mouse BA/F3 cells NHnWR5RRem:uaX\ldoF1cW:wIHHzd4F6 MUXBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IH3veZNmKEKDL1[zJINmdGy|IITyZY5{\mWldHXkJJdqfGhiRVfGVkBGPzR4X1G3OVBg\GWuL2S3PVBOKG23dHHueEwhTUN3ME2yJI5O MXKyNVIxQDhyMh?=
human HCC827 cells M{nOcnBzd2yrZnXyZZRqd25iYYPzZZk> Mnn4O|IhcA>? MlHwRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCKQ1O4Nlch[2WubIOgbIFz[m:{aX7nJGVITlJiZHXsJGU4PDZvQUe1NEBufXSjboSgZYZ1\XJiN{KgbJJ{KGK7IF3UV{Bie3OjeTygTWM2OD15IH7N M1PlXFIzOzN7M{Sy
human PC9 cells NFfpb4VRem:uaX\ldoF1cW:wIHHzd4F6 M4nPR2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4Sg[5Jwf3SqLYLld4l{fGGwdDDoeY1idiCSQ{mgZ4VtdHNiZYjwdoV{e2mwZzDFS2ZTKEV5NE\fRVc2OC:WN{mwUUBufXSjboSsJGVEPTB;MUSgcm0> MmmyNlEzODh6MEK=
NCI-H1975 cells M3HVbWZ2dmO2aX;uJIF{e2G7 MXGyJIg> M3fofGlvcGmkaYTpc44hd2ZiRVfGVkBNQDV6Uj;UPVcxVSCmb4XicIUhdXW2YX70JJBpd3OyaH;yfYxifGmxbjDpckBpfW2jbjDOR2kuUDF7N{WgZ4VtdHNiYX\0[ZIhOiCqcoOgZpkh\my3b4Lld4NmdmOnIHHzd4F6NCCLQ{WwQVAvODJ|IN88US=> MkCwNlM6OzB7OUS=
human 16HBE cells M1jHSnBzd2yrZnXyZZRqd25iYYPzZZk> MknLO|IhcA>? MmjJRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiBzNljCSUBk\WyuczDlfJBz\XO|aX7nJJdqdGRidInw[UBGT0[UIHHmeIVzKDd{IHjyd{BjgSCPVGSgZZN{[XluIFnDOVA:OC56MUGg{txO MVWyN|c6OjNzOB?=
human A431 cells MoWxR5l1d3SxeHnjbZR6KGG|c3H5 MUG3NkBp M{fxcmN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGE1OzFiY3XscJMhd3[ncnX4dJJme3Orbnege4lt\CC2eYDlJGVITlJiYYPz[ZN{\WRiYYOg[5Jwf3SqIHnubIljcXSrb36gZYZ1\XJiN{KgbJJ{KGK7IF3UWEBie3OjeTygTWM2OD1zLkGwPEDPxE1? M3jyPFI{PjZ6NESx
human LoVo cells MXXGeY5kfGmxbjDhd5NigQ>? MUiyJIg> NVHEWJpRUW6qaXLpeIlwdiCxZjD3bYxlKHS7cHWgSWdHWiCyaH;zdIhwenmuYYTpc44hcW5iaIXtZY4hVG:YbzDj[YxteyCjZoTldkAzKGi{czDifUBndHWxcnXzZ4Vv[2ViYYPzZZktKEmFNUC9NU4yQCEQvF2= NIDJUlMzOzl|MEm5OC=>
human 16HBE14o- cells  NVXqc3N4S3m2b4TvfIlkcXS7IHHzd4F6 NHfQd4Q4OiCq NUHuZ41OS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hOT[KQlWxOI8uKGOnbHzzJIhiemKxcnnu[{B4cWymIIT5dIUhTUeIUjDhd5Nme3OnZDDhd{Boem:5dHigbY5pcWKrdHnvckBi\nSncjC3NkBpenNiYomgUXRVKGG|c3H5MEBKSzVyPUGuN|U2KM7:TR?= NX\RbIZiOjN4Nki0OFE>
human BEAS2B cells M1PRW2N6fG:2b4jpZ4l1gSCjc4PhfS=> NWjYN3R[PzJiaB?= NXzST455S3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hSkWDU{LCJINmdGy|IHjhdoJwemmwZzD3bYxlKHS7cHWgSWdHWiCjc4Pld5Nm\CCjczDndo94fGhiaX7obYJqfGmxbjDh[pRmeiB5MjDodpMh[nliTWTUJIF{e2G7LDDJR|UxRTFwOEGxJO69VQ>? NX\ZclR3OjN4Nki0OFE>
human A549 cells M4C2XnBzd2yrZnXyZZRqd25iYYPzZZk> NX;QTW1IPzJiaB?= MmXHRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDrMXJCWyCmZYDlcoRmdnRiaIXtZY4hSTV2OTDj[YxteyCxdnXy[ZhxemW|c3nu[{BYXCCHR1\SJIFnfGW{IEeyJIhzeyCkeTDNWHQh[XO|YYmsJGlEPTB;Mj6xNFIh|ryP Ml3yNlQ3ODd3OUG=
human HL7702 cells NFP1T3RRem:uaX\ldoF1cW:wIHHzd4F6 MXS3NkBp M3HXOWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iSFy3O|AzKGOnbHzzJIV5eHKnc4Ppcochf2mudDD0fZBmKEWJRmKgZYZ1\XJiN{KgbJJ{KGK7IF3UV{Bie3OjeTygTWM2OD1{LkezJO69VQ>? MnHsNlI{Ozl|NEK=


体内試験 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]


+ 展開

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.
細胞試験: [1]
+ 展開
  • 細胞株: NSCLC, Ba/F3 cells, NIH-3T3 cells, PC9GR4 cells
  • 濃度: 0-1 μM
  • 反応時間: 72 hours
  • 実験の流れ: 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.
+ 展開
  • 動物モデル: EGFR-TL (T790M/L858R) mice
  • 製剤: NMP (10% 1-methyl-2-pyrrolidinone: 90% PEG-300
  • 投薬量: 25mg/kg
  • 投与方法: Gavage

溶解度 (25°C)

体外 DMSO 13 mg/mL (26.3 mM)
Water Insoluble
Ethanol Insoluble
体内 左から(NMPから)右の順に溶剤を製品に加えます(文献ではなく、Selleckの実験によるデータ):
30% PEG400+0.5% Tween80+5% propylene glycol
30 mg/mL

* 溶解度測定はSelleck技術部門によって行われており、その他文献に示されている溶解度と差異がある可能性がありますが、同一ロットの生産工程で起きる正常な現象ですからご安心ください。


分子量 494.18


CAS No. 1213269-23-8
in solvent
別名 N/A





質量 (g) = 濃度 (mol/L) x 体積 (L) x 分子量 (g/mol)


  • 質量





開始濃度 x 開始体積 = 最終濃度 x 最終体積


この方程式は、一般に略語を使われます:C1V1 = C2V2 ( 入力 出力 )

  • C1



  • 連続希釈剤

  • 計算結果

  • 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):




チップス: 化学式は大文字と小文字の区別ができます。C10H16N2O2 c10h16n2o2


質量 濃度 体積 分子量



Handling Instructions


  • * 必須


EGFR Inhibitors with Unique Features


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細胞株 試験類型 濃度 培養時間 溶剤類型 活性叙述 PMID