5.30536

EGFR Activator, NSC 228155

• Synonym(s): 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
• Empirical Formula (Hill Notation): C₁₁H₆N₄O₄S
• CAS Number: 113104-25-9
• Molecular Weight: 290.25
• UNSPSC Code: 41121801
• NACRES: NA.77

Properties

• Assay: ≥97% (HPLC)
• Quality Level: 100
• 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

Description

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.

Biochem/physiol Actions

Cell permeable: yes

Primary Target
EGF receptor

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.

Use only fresh DMSO for reconstitution.

Other Notes

Sakanyan, V., et al. 2014. Sci. Rep.4, 3977.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Safety Information

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 3
• Flash Point(F): Not applicable
• Flash Point(C): Not applicable