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SML1168

Sigma-Aldrich

WZ4002

≥98% (HPLC)

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

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

Biochem/physiol Actions

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.

WGK

WGK 3

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable

Regulatory Information

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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
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
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
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
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)
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