EGFR-kinase inhibitor
     
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EGFR-kinase inhibitor

N-(3-Bromophenyl)-6,7-dimethoxy-4-quinazolinamine hydrochloride (AG 1517; NSC 669364; PD 153035; SU 5271; WHI-P79)
extremely potent inhibitor of epidermal growth factor (EGF) receptor tyrosine kinase, with an IC50 of 25 pM. Inhibits other purified tyrosine kinases only at micromolar or higher concentrations

EGFR-kinase_inhibitor
OTAVAchemicals Catalogue Number: 7020540711
CAS Registry Number: 153436-54-5
Purity: 95%+ (HPLC)


Ref.: Grunt et al. An EGF receptor inhibitor induces RAR-? expression in breast and ovarian cancer cells. Biochemical and Biophysical Research Communications (2005), 329, 1253-1259


Abstract: Inhibition of the epidermal growth factor (EGF)-receptor (EGFR) has become a promising anticancer treatment strategy. Application of retinoids yields encouraging results for cancer prevention and therapy. Many tumors express no or low amounts of retinoic acid receptor-?2 (RAR-?2) due to epigenetic silencing via DNA hypermethylation. RAR-?2 is the main mediator of the antiproliferative effect of retinoids. RAR-?2 re-expression causes reversal of transformation, cell cycle arrest, and restoration of retinoid sensitivity. RAR-?2 is thus a tumor suppressor. Western blotting, colorimetric in vitro cell proliferation assays, and reverse transcription-polymerase chain reaction demonstrated that the EGFR inhibitor PD153035 not only blocked activation of EGFR and inhibited cell growth, but also stimulated RAR-? expression in MDA-MB-468 breast and OVCAR-3 ovarian carcinoma cells. Upregulation of RAR-? by PD153035 was confirmed by real-time reverse transcription-polymerase chain reaction. In contrast, expression of other retinoid receptors and of estrogen receptor-? was not affected. PD153035-mediated re-induction of RAR-? was associated with demethylation of the RAR-?2 gene promoter P2 as demonstrated by methylation-specific polymerase chain reaction. These novel results on the ErbB/retinoid receptor cross-talk may be useful for designing future anticancer combination regimens.

 
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