5.30536
EGFR Activator, NSC 228155
别名:
EGFR Activator, NSC 228155, 4-Nitro-7-((1-oxidopyridin-2-yl)sulfanyl)-2,1,3-benzoxadiazole, 4-Nitro-7-(1-oxy-pyridin-2-ylsulfanyl)-benzo[1,2,5]oxadiazole, 2-(7-Nitrobenzo[c][1,2,5]oxadiazol-4-ylthio)pyridine-1-oxide, NSC-228155
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关于此项目
经验公式（希尔记法）:
C11H6N4O4S
化学文摘社编号:
分子量:
290.25
MDL number:
UNSPSC Code:
41121801
NACRES:
NA.77
Assay:
≥97% (HPLC)
Form:
powder
Quality level:
Storage condition:
OK to freeze
desiccated (hygroscopic)
protect from light
desiccated (hygroscopic)
protect from light
InChI key
ICCFXXDUYSPKOL-UHFFFAOYSA-N
SMILES string
S(c3[n+](cccc3)[O-])c1c2n[o]nc2c(cc1)[N+](=O)[O-]
assay
≥97% (HPLC)
form
powder
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze
desiccated (hygroscopic)
protect from light
color
burnt orange
solubility
DMSO: 5 mg/mL
storage temp.
2-8°C
Quality Level
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Biochem/physiol Actions
Cell permeable: yes
Primary Target
EGF receptor
EGF receptor
Disclaimer
Toxicity: Standard Handling (A)
General description
A nitro-benzoxadiazole (NBD) compound that directly binds to the dimerization domain of sEGF receptor to generate stable dimers and allosterically activates the receptor. Exhibits similar phosphorylation profile as the cognate EGF-ligand. Enhances the phosphorylation of Tyr1068 and Tyr1173 in MDA-MB-468 cells in a time- and dose-dependent manner (EC50 = 52 µM with respect to Tyr1068). These phosphorylation events can be blocked by pre-incubating cells with AG1478 (>Cat. No. 658852; 10 µM) or PD153035 (https://www.emdmillipore.com/US/en/product/Complement-C9-Depleted-Serum-Human,EMD_BIO-234409">>Cat. No. 234490; 2 µM) that selectively block the ATP-binding pocket of EGFR. Tyr1068 phosphorylation of the receptor can also be completely blocked in EGF treated MDA-MB-468 cells exposed to anti-EGFR neutralizing antibody.
Other Notes
Sakanyan, V., et al. 2014. Sci. Rep.4, 3977.
Packaging
Packaged under inert gas
Preparation Note
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Use only fresh DMSO for reconstitution.
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
Vehary Sakanyan et al.
Scientific reports, 4, 3977-3977 (2014-02-06)
Peptide ligand-induced dimerization of the extracellular region of the epidermal growth factor receptor (sEGFR) is central to the signal transduction of many cellular processes. A small molecule microarray screen has been developed to search for non-peptide compounds able to bind
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