Lapatinib

Biological Activity

Lapatinib is a potent and selective dual ErbB2 (HER-2) and EGFR inhibitor (IC₅₀ values are 9.8 and 10.2 nM, respectively). Selective for EGFR and ErbB-2 versus other proliferative kinases. Inhibits proliferation in multiple cancer cell lines (average IC₅₀ values <0.16 μM). Exhibits 100-fold average selectivity for the tumor cells versus human foreskin fibroblasts. Inhibits EGFR/ErbB2 autophosphorylation and phosphorylation of the downstream modulator AKT.

Technical Data

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Background References

1. The effects of the novel, reversible epidermal growth factor receptor/ErbB-2 tyrosine kinase inhibitor, GW2016, on the growth of human normal and tumor-derived cell lines in vitro and in vivo.
   Rusnak et al.
   Mol.Cancer Ther., 2001;1:85

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