EGFR/Erbb2 Inhibitor

Decent Essays
C3285

Description:
IC50: 20 and 79 nM for EGFR and c-ErbB2, respectively

EGFR/ErbB2 Inhibitor is an EGFR and c-ErbB2 inhibitor.

EGFR and c-ErbB-2 are members of the epidermal growth factor receptor subfamily of protein tyrosine kinases. Their cellular overexpression causes transformation, so that the cells will grow in the absence of growth factors. An inhibitor of thse kinases should block the receptor signalling, subsequent transformation and inappropriate growth.

In vitro: EGFR/ErbB2 Inhibitor was identified as a potent inhibitor of both c-erbB-2 and EGFr [IC50: 0.079 μM for c-erbB-2, 0.020 μM for EGFr (isolated enzyme), 2.0 μM for HB4aC5.2 cells, 1.2 μM for BT474, both overexpressing c-erbB-2; 2.5 μM for HN5 cells overexpressing EGFr].

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