EGF816 Struktur

EGF816

Bezeichnung:EGF816

CAS-Nr1508250-71-2

Englisch Name:EGF816

CBNumberCB33040785

SummenformelC26H31ClN6O2

Molgewicht495.02

MOL-Datei1508250-71-2.mol

EGF816 physikalisch-chemischer Eigenschaften

Dichte	1.28±0.1 g/cm3(Predicted)
storage temp.	Store at -20°C
Löslichkeit	Soluble in DMSO
Aggregatzustand	Powder
pka	11.38±0.43(Predicted)

Gefahreninformationscode (GHS)

EGF816 Chemische Eigenschaften,Einsatz,Produktion Methoden

Beschreibung
Nazartinib is an irreversible inhibitor of mutant EGF receptors (EGFRs). It is selective for EGFR mutant cell lines, including H3255 and HCC827 lung adenocarcinoma cells (IC₅₀s = 6.11 and 1.52 nM, respectively) and resistant H1975 non-small cell lung cancer cells (NSCLC; IC₅₀ = 4.18 nM), over cells expressing wild-type EGFRs (IC₅₀ = 160.6 nM for HaCaT keratinocytes). Nazartinib decreases phosphorylation of EGFR in H3255, HCC827, and H1975 cells (EC₅₀s = 5, 1, and 3 nM, respectively) and inhibits cell proliferation (EC₅₀s = 9, 11, and 25 nM, respectively) but does not affect cell proliferation in cell lines containing wild-type EGFR. It reduces tumor growth in an HCC827 lung adenocarcinoma mouse xenograft model when administered at doses ranging from 3 to 100 mg/kg per day for 21 days.
in vitro
egf816 showed sustained inhibition of pegfr, which is consistent with the irreversible binding mechanism of egf816. egf816 also performs exceptionally well in long term dosing studies providing durable responses in the preclinical models [1].
in vivo
egf816 demonstrated strong in vivo tumor regressions in several egfr activating and resistant tumor models. in all of the models egf816 inhibited tumor growth dose-dependently and achieved regressions of established tumors at well tolerated doses [1].
Einzelnachweise
[1] shailaja kasibhatla, jie li, celin tompkins, mei-ting vaillancourt, jennifer anderson, annemarie culazzo pferdekamper, chun li, oliver long, mathew mcneill, robert epple, debbie liao, eric murphy, steve bender, yong jia, gerald lelais. egf816, a novel covalent inhibitor of mutant-selective epidermal growth factor receptor, overcomes t790m-mediated resistance in nsclc. [abstract]. in: proceedings of the 105th annual meeting of the american association for cancer research; 2014 apr 5-9; san diego, ca. philadelphia (pa): aacr; cancer res 2014;74(19 suppl):abstract nr 1733. doi:10.1158/1538-7445.am2014-1733

EGF816 Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

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