341216
NSC668394
≥95% (HPLC), solid, Ezrin inhibitor, Calbiochem®
Synonyme(s) :
Ezrin Inhibitor, NSC668394, 7-(3,5-dibromo-4-hydroxyphenethylamino)quinoline-5,8-dione
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About This Item
Formule empirique (notation de Hill):
C17H12Br2N2O3
Numéro CAS:
Poids moléculaire :
452.10
Numéro MDL:
Code UNSPSC :
12352200
Nomenclature NACRES :
NA.77
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product name
Ezrin Inhibitor, NSC668394, The Ezrin Inhibitor, NSC668394 controls the biological activity of Ezrin.
Niveau de qualité
Pureté
≥95% (HPLC)
Forme
solid
Fabricant/nom de marque
Calbiochem®
Conditions de stockage
OK to freeze
protect from light
Couleur
red-orange
Solubilité
DMSO: 50 mg/mL, clear, red-orange
Conditions d'expédition
ambient
Température de stockage
−20°C
Chaîne SMILES
O=C1C=C(NCCC2=CC(Br)=C(O)C(Br)=C2)C(C3=C1C=CC=N3)=O
Description générale
A cell-permeable, quinoline that binds directly to ezrin (Kd = 12.6 µM) in a reversible manner, and inhibits PKCι-mediated ezrin phosphorylation at Thr567 (IC50 = 8.1 µM) and ezrin-actin binding, in vitro. It also inhibits murine osteosarcoma K7M2 cell invasion in a monolayer of HUVEC cells, dose-dependently, from 1 to 10 µM. At 10 µM, it causes a unique developmental defect in zebrafish, characterized by reduced motility of eye progenitor cells. Furthermore, this small molecule prevents metastatic growth in an ex vivo mouse lung organ culture assay at 10 µM and attenuates ezrin-dependent OS metastatic growth in mouse lung model in vivo at 2.26 mg/kg/day.
A cell-permeable, quinoline that binds directly to ezrin (Kd = 12.6 µM) in a reversible manner, and inhibits PKCι-mediated ezrin phosphorylation at Thr567 (IC50 = 8.1 µM) and ezrin-actin binding, in vitro. It also inhibits murine osteosarcoma K7M2 cell invasion in a monolayer of HUVEC cells, dose-dependently, from 1 to 10 µM. At 10 µM, it causes a unique developmental defect in zebrafish, characterized by reduced motility of eye progenitor cells. Furthermore, this small molecule prevents metastatic growth in an ex vivo mouse lung organ culture assay at 10 µM and attenuates ezrin-dependent OS metastatic growth in mouse lung model in vivo at 2.26 mg/kg/day.
Conditionnement
Packaged under inert gas
Avertissement
Toxicity: Standard Handling (A)
Reconstitution
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Autres remarques
Bulut, G., et al. 2011. Oncogene31, 269.
Informations légales
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Code de la classe de stockage
11 - Combustible Solids
Classe de danger pour l'eau (WGK)
WGK 2
Point d'éclair (°F)
Not applicable
Point d'éclair (°C)
Not applicable
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