Skip to Content
Merck
CN

SML1168

WZ4002

≥98% (HPLC)

Synonym(s):

N-[3-[[5-Chloro-2-[[2-methoxy-4-(4-methyl-1-piperazinyl)phenyl]amino]-4-pyrimidinyl]oxy]phenyl]-2-propenamide, WZ-4002

Sign In to View Organizational & Contract Pricing

Select a Size

About This Item

Empirical Formula (Hill Notation):
C25H27ClN6O3
CAS Number:
1213269-23-8
Molecular Weight:
494.97
MDL number:
MFCD16621244
UNSPSC Code:
12352202
PubChem Substance ID:
329825698
NACRES:
NA.77

Key Documents

View All Documentation
Technical Service
Need help? Our team of experienced scientists is here for you.
Let Us Assist
Technical Service
Need help? Our team of experienced scientists is here for you.
Let Us Assist

Quality Level

100

Assay

≥98% (HPLC)

form

powder

color

white to beige

solubility

DMSO: 5 mg/mL, clear (warmed)

storage temp.

−20°C

SMILES string

CN(CC1)CCN1C2=CC(OC)=C(NC3=NC=C(Cl)C(OC4=CC(NC(C=C)=O)=CC=C4)=N3)C=C2

InChI

1S/C25H27ClN6O3/c1-4-23(33)28-17-6-5-7-19(14-17)35-24-20(26)16-27-25(30-24)29-21-9-8-18(15-22(21)34-3)32-12-10-31(2)11-13-32/h4-9,14-16H,1,10-13H2,2-3H3,(H,28,33)(H,27,29,30)

InChI key

ITTRLTNMFYIYPA-UHFFFAOYSA-N

Related Categories

Biochem/physiol Actions

WZ4002 is an irreversible inhibitor of the gatekeeper EGFR-T790M kinase.
WZ4002 is an irreversible inhibitor of the gatekeeper EGFR-T790M mutation that binds to the active conformation of the EGFR kinase forming a covalent bond with Cys 797.
WZ4002 is effective in the treatment of lung adenocarcinomas due to EGFR (epidermal growth factor receptor) mutations.

Storage Class Code

11 - Combustible Solids

WGK

WGK 3

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable

Regulatory Information

新产品
This item has

Choose from one of the most recent versions:

Certificates of Analysis (COA)

Lot/Batch Number
0000150560
0000150559
0000150559
0000150560
035M4787V

Don't see the Right Version?

If you require a particular version, you can look up a specific certificate by the Lot or Batch number.

Search for a COA

Already Own This Product?

Find documentation for the products that you have recently purchased in the Document Library.

Visit the Document Library

Jin Kyung Rho et al.
Cancer research, 77(5), 1200-1211 (2017-01-14)
The clinical utility of approved EGFR small-molecule kinase inhibitors is plagued both by toxicity against wild-type EGFR and by metastatic progression in the central nervous system, a disease sanctuary site. Here, we report the discovery and preclinical efficacy of GNS-1486
Francesca Iommelli et al.
Clinical cancer research : an official journal of the American Association for Cancer Research, 24(13), 3126-3136 (2018-04-06)
Purpose: Our aim was to test whether imaging with 18F-fluorothymidine (18F-FLT) PET/CT was able to detect the combined effects of EGFR and MET inhibitors in oncogene-driven non-small cell lung cancer (NSCLC) and to elucidate the mechanisms underlying the enhanced efficacy
WZ4002, a third-generation EGFR inhibitor, can overcome anoikis resistance in EGFR-mutant lung adenocarcinomas more efficiently than Src inhibitors.
Sakuma Y, et al.
Laboratory Investigation; a Journal of Technical Methods and Pathology, 92(3), 371-371 (2012)
Xiao Xu et al.
Molecular cancer therapeutics, 15(11), 2586-2597 (2016-11-04)
AC0010 is a pyrrolopyrimidine-based irreversible EGFR inhibitor, structurally distinct from previously reported pyrimidine-based irreversible EGFR inhibitors, such as osimertinib and rociletinib. AC0010 selectively inhibits EGFR-active and T790M mutations with up to 298-fold increase in potency compared with wild-type EGFR. In
Sujin Kim et al.
Biochemical and biophysical research communications, 503(2), 710-714 (2018-06-18)
The emergence of the T790M gatekeeper mutation in the Epidermal Growth Factor Receptor (EGFR) gene is an important mechanism that can lead to the acquired resistance to EGFR-targeted tyrosine kinase inhibitors such as erlotinib or gefitinib. These drugs have been
View All Related Papers

Our team of scientists has experience in all areas of research including Life Science, Material Science, Chemical Synthesis, Chromatography, Analytical and many others.

Contact Technical Service