Description

Patients with non-small-cell lung cancer (NSCLC) with somatic activating mutations of the epidermal growth factor receptor gene (EGFR mutations) generally respond to EGFR tyrosine kinase inhibitors (EGFR-TKIs). β-Catenin is a key component of the Wnt/β-Catenin signal and is an important oncogene that is involved in pathogenesis and progression of malignant tumors, especially cancer stem cells. It was found that EGFR-mutated NSCLC cell lines exhibited a high expression level of β-Catenin, compared with cell lines with the wild-type EGFR gene, and XAV939 (a β-Catenin inhibitor) enhanced the sensitivities to EGFR-TKI in EGFR-mutated NSCLC cell lines.

In EGFR-mutated NSCLC cell lines with acquired resistance threonine-to-methionine mutation in codon 790 (T790M) mutation, XAV939 enhanced the sensitivity of the cells to an irreversible EGFR-TKI but not a reversible EGFR-TKI. The combination of XAV939 and EGFR-TKIs strongly inhibited the β-Catenin signal and strongly decreased the phosphorylation of EGFR, compared with the use of EGFR-TKIs alone, suggesting an interaction between EGFR and the β-Catenin signal. The stem cell-like properties of the EGFR-mutated cell line carrying the T790M mutation were inhibited by XAV939 and BIBW2992 (an irreversible EGFR-TKI). Furthermore, the stem cell-like properties were strongly inhibited by a combination of both the agents. A xenograft study demonstrated that β-Catenin knockdown enhanced the antitumor effect of BIBW2992 in the EGFR-mutated NSCLC cell line carrying the T790M mutation. Conclusion: The findings indicate that β-Catenin might be a novel therapeutic target in EGFR-mutated NSCLC carrying the T790M mutation.

4-Chloro-6,7-dimethoxyquinazoline(13790-39-1) Specifications

CAS	13790-39-1
CAS Min %	95.0
CAS Max %	100.0
MDL Number	MFCD01570172
InChI Key	LLLHRNQLGUOJHP-UHFFFAOYSA-N
Chemical Name or Material	4-Chloro-6,7-dimethoxyquinazoline
Infrared Spectrum	Authentic
Physical Form	Powder or Chunks
Packaging	Glass bottle
Molecular Formula	C10H9ClN2O2
Molecular Weight (g/mol)	224.65
SMILES	COC1=C(C=C2C(=C1)C(=NC=N2)Cl)OC
Color	White or almost white power
Melting Point	184-187°C
Assay	98%

 

4-Chloro-6,7-dimethoxyquinazoline(13790-39-1) Safety and Handling

(13790-39-1) Hazard description:

♦ Causes skin irritation.

♦ Causes serious eye irritation.

♦ May cause respiratory irritation.

(13790-39-1) Precautionary statement:

♦ Avoid breathing dust/fume/gas/mist/vapors/spray.

♦ Wear protective gloves/protective clothing/eye protection/face protection.

♦ IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continue rinsing.

♦ IF INHALED: Remove to fresh air and keep at rest in a position comfortable for breathing.

♦ Store locked up.

♦ Dispose of contents/container in accordance with local/regional/national/international regulations.

WARNING: The information provided on this web site was developed in compliance with European Union (EU) regulations and is correct to the best of our knowledge, information and belief at the date of its publication. The information given is designed only as a guide for safe handling and use. It is not to be considered as either a warranty or quality specification.

4-Chloro-6,7-dimethoxyquinazoline(13790-39-1) Articles

R K Narla; X P Liu; D E Myers; and F M Uckun. 4-(3′-Bromo-4’hydroxylphenyl)-amino-6,7-dimethoxyquinazoline: a novel quinazoline derivative with potent cytotoxic activity against human glioblastoma cells. Clin Cancer Res. 1988, 41405.

Chappie, T.A, et.al. Discovery of a Series of 6,7-Dimethoxy-4-pyrrolidylquinazoline PDE10A Inhibitors†.J. Med. Chem. 2007 , 50(2), 182-185.

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