EGFR ACTIVATOR NSC 228155 (C15-1305-016)

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

Molecular Weight: 290.25. Empirical Formula: C₁₁H₆N₄O₄S. 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. Storage Class Code: 11 - Combustible Solids. WGK: WGK 3. Flash Point(F): Not applicable. Flash Point(C): Not applicable.