EGFR/ErbB-2 Inhibitor

A cell-permeable 4-anilino quinazoline compound that acts a potent, reversible, and ATP-competitive inhibitors of EGFR and c-erbB2 (IC₅₀ = 20 nM and 79 nM, respectively), members of the type I growth factor receptor family that is involved in breast cancer development and progression. Shown to effectively inhibit the proliferation (IC₅₀ = ~ 1.2-2.5 µM) of tumor cells overexpressing EGRF or c-erbB-2.

A cell-permeable, potent, reversible, and ATP-competitive inhibitor of the tyrosine kinase activity of EGFR (IC₅₀ = 20 nM) and c-erbB2 (IC₅₀ = 79 nM), members of the type I growth factor receptor family implicated in the development and progression of various forms of cancer, including breast and small lung cell carcinoma. Shown to effectively inhibit the proliferation (IC₅₀ ~1.2-2.5 µM) of tumor cells overexpressing EGRF or c-erbB-2.

Cell permeable: yes

Primary Target
EGFR

Product competes with ATP.

Reversible: yes

Target IC₅₀: 20 nM and 79 nM, against EGFR and c-erbB2, respectively

Packaged under inert gas

Toxicity: Carcinogenic / Teratogenic (D)

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Cockerill, S., et al. 2001. Bioorg. Med. Chem. Lett.11, 1401.

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