341216
NSC668394
≥95% (HPLC), solid, Ezrin inhibitor, Calbiochem®
Sinónimos:
Ezrin Inhibitor, NSC668394, 7-(3,5-dibromo-4-hydroxyphenethylamino)quinoline-5,8-dione
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About This Item
Fórmula empírica (notación de Hill):
C17H12Br2N2O3
Número de CAS:
Peso molecular:
452.10
MDL number:
UNSPSC Code:
12352200
NACRES:
NA.77
Productos recomendados
product name
Ezrin Inhibitor, NSC668394, The Ezrin Inhibitor, NSC668394 controls the biological activity of Ezrin.
Quality Level
assay
≥95% (HPLC)
form
solid
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze
protect from light
color
red-orange
solubility
DMSO: 50 mg/mL, clear, red-orange
shipped in
ambient
storage temp.
−20°C
SMILES string
O=C1C=C(NCCC2=CC(Br)=C(O)C(Br)=C2)C(C3=C1C=CC=N3)=O
General description
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.
Packaging
Packaged under inert gas
Warning
Toxicity: Standard Handling (A)
Reconstitution
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Other Notes
Bulut, G., et al. 2011. Oncogene31, 269.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Storage Class
11 - Combustible Solids
wgk_germany
WGK 2
flash_point_f
Not applicable
flash_point_c
Not applicable
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