GSK6853 Struktur

GSK6853

Bezeichnung:GSK6853

CAS-Nr1910124-24-1

Englisch Name:GSK6853

CBNumberCB73145989

SummenformelC22H27N5O3

Molgewicht409.48

MOL-Datei1910124-24-1.mol

GSK6853 physikalisch-chemischer Eigenschaften

Siedepunkt	545.9±50.0 °C(Predicted)
Dichte	1.247±0.06 g/cm3(Predicted)
storage temp.	Sealed in dry,Store in freezer, under -20°C
Löslichkeit	Soluble in DMSO (25 mg/ml); ethanol (25 mg/ml)
Aggregatzustand	solid
pka	13.03±0.20(Predicted)
Farbe	White
Optische Aktivität	[α]/D -45 to -55°, c =0.3 in methanol
Stabilität	Stable for 1 year from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20°C for up to 3 months.

GSK6853 Chemische Eigenschaften,Einsatz,Produktion Methoden

Beschreibung
GSK6853 (1910124-24-1) is a very potent (pIC50 = 8.6 vs full length protein, 7.7 in cellular assays) inhibitor of Bromodomain and PHD Finger-containing 1 (BRPF1). It displayed >1600-fold selectivity over other bromodomains.
Verwenden
N-[2,3-Dihydro-1,3-dimethyl-6-[(2R)-2-methyl-1-piperazinyl]-2-oxo-1H-benzimidazol-5-yl]-2-methoxybenzamide can be used in biological study of preparation of bromodomain and PHD finger-containing protein inhibitors.
in vitro
in previous study, gsk6853 was tested in the bromoscan panel of bromodomain binding assays and the results showed that consistent with the previous findings, it showed excellent brpf1 potency (pkd 9.5) and greater than 1600-fold selectivity over all other bromodomains tested. in addition, screening gsk6853 against a panel of 48 unrelated assays revealed only off-target activities that were relatively weak compared to its high brpf1 potency [1].
in vivo
to assess the suitability of gsk6853 for in vivo studies, its dmpk characteristics were studied in male cd1 mice by i.v., po, and i.p. administration. the results indicated that the i.p. route of administration would be suitable for dosing this molecule in further pk/pd models. moreover, in order to be able to compare biochemical potency measurements to free blood concentrations, the fraction unbound in the cd1 mouse was also tested with a resulting value of 7.9% [1].
Lager
Store at -20°C
Einzelnachweise
Bamborough et al. (2016), GSK6853, a Chemical Probe for Inhibition of the BRPF1 Bromodomain; ACS Med.Chem. Lett. 7 552

GSK6853 Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

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