EGFR Activator, NSC 228155-Calbiochem

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一般描述

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 ?M with respect to Tyr1068). These phosphorylation events can be blocked by pre-incubating cells with AG1478 (>Cat. No. 658852; 10 ?M) or PD153035 (>Cat. No. 234490; 2 ?M) 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.
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 ?M with respect to Tyr1068). These phosphorylation events can be blocked by pre-incubating cells with AG1478 (>Cat. No. 658852; 10 ?M) or PD153035 (>Cat. No. 234490; 2 ?M) 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.

Please note that the molecular weight for this compound is batch-specific due to variable water content.

生化/生理作用

Cell permeable: yes
Primary Target
EGF receptor

包装

Packaged under inert gas

警告

Toxicity: Standard Handling (A)

重悬

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.

其他说明

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

法律信息

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

基本信息

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