4-(3-Chloro-4-fluorophenylamino)-7-methoxy-6-[3-(4-morpholinyl)propoxy]quinazoline hydrochloride Struktur

4-(3-Chloro-4-fluorophenylamino)-7-methoxy-6-[3-(4-morpholinyl)propoxy]quinazoline hydrochloride

Bezeichnung:4-(3-Chloro-4-fluorophenylamino)-7-methoxy-6-[3-(4-morpholinyl)propoxy]quinazoline hydrochloride

Englisch Name:4-(3-Chloro-4-fluorophenylamino)-7-methoxy-6-[3-(4-morpholinyl)propoxy]quinazoline hydrochloride

CBNumberCB12128725

SummenformelC22H25Cl2FN4O3

Molgewicht483.37

4-(3-Chloro-4-fluorophenylamino)-7-methoxy-6-[3-(4-morpholinyl)propoxy]quinazoline hydrochloride physikalisch-chemischer Eigenschaften

storage temp.	Store at -20°C
Löslichkeit	insoluble in EtOH; ≥4.28 mg/mL in H2O with gentle warming and ultrasonic; ≥6.9 mg/mL in DMSO with gentle warming
Aggregatzustand	Powder
Farbe	White to off-white

4-(3-Chloro-4-fluorophenylamino)-7-methoxy-6-[3-(4-morpholinyl)propoxy]quinazoline hydrochloride Chemische Eigenschaften,Einsatz,Produktion Methoden

Biologische Aktivität
the egfr is a mr 170,000 transmembrane glycoprotein with an external binding domain and an intracellular tyrosine kinase domain. gefitinib (zd-1839, iressa) is an epidermal growth factor receptor-selective tyrosine kinase inhibitor.
in vitro
gefitinib inhibited colony formation in soft agar in a dose dependent manner in all cancer cell lines. however, treatment with higher doses resulted in a 2–4-fold increases in apoptosis. dose-dependent supra-additive increase in growth inhibition was observed when cancer cells were treated with totoxic drugs and gefitinib. the combined treatment markedly enhanced apoptotic cell death induced by single agent treatment [1].
in vivo
gefitinib treatment of nude mice bearing established human geo colon cancer xenografts revealed a reversible dose-dependent inhibition of tumor growth because geo tumors resumed the growth rate of controls at the end of the treatment [1].
target

Target Value
EGFR
(Cell-free assay) 15.5 nM
EGFR (858R/T790M)
(Cell-free assay) 823.3 nM
Einzelnachweise
[1] ciardiello f, caputo r, bianco r, damiano v, pomatico g, de placido s, bianco ar, tortora g. antitumor effect and potentiation of cytotoxic drugs activity in human cancer cells by zd-1839 (iressa), an epidermal growth factor receptor-selective tyrosine kinase inhibitor. clin cancer res. 2000;6(5):2053-63.
[2] cantarini mv, mcfarquhar t, smith rp, bailey c, marshall al. relative bioavailability and safety profile of gefitinib administered as a tablet or as a dispersion preparation via drink or nasogastric tube: results of a randomized, open-label, three-period crossover study in healthy volunteers. clin ther. 2004;26(10):1630-6.

4-(3-Chloro-4-fluorophenylamino)-7-methoxy-6-[3-(4-morpholinyl)propoxy]quinazoline hydrochloride Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

184475-55-6, 4-(3-Chloro-4-fluorophenylamino)-7-methoxy-6-[3-(4-morpholinyl)propoxy]quinazoline hydrochloride Verwandte Suche:

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Target	Value
EGFR (Cell-free assay)	15.5 nM
EGFR (858R/T790M) (Cell-free assay)	823.3 nM