Lapatinib, 10 mg

A selective dual tyrosine kinase inhibitor from STEMCELL Technologies, this small molecule (also known as Tykerb) targets the epidermal growth factor receptor (EGFR, ErbB1) and human epidermal growth factor receptor 2 (HER2, ErbB2) [S1][S2]. It binds reversibly to the ATP binding pocket in an inactive-like conformation with a very slow off-rate, thereby preventing autophosphorylation [S1].

In published cancer research, the compound induces apoptosis in cells overexpressing EGFR and/or HER2 and inhibits tumor growth in a mouse xenograft model [S1][S2]. Reported IC50 values for EGFR and HER2 are each about 10 nM, with corresponding Ki values of 3 and 13 nM [S1]. The molecular weight is 581.1 g/mol and the purity is ≥ 98% [S1].

Supplied as a crystalline solid, the compound is soluble in DMSO at concentrations up to 30 mM [S1]. For use as a cell culture supplement, stock solution should be diluted into culture medium immediately before use, with final DMSO concentration kept below 0.1% to avoid potential cell toxicity [S1]. The product is stable at -20°C as supplied for 12 months from the date of receipt and should be protected from prolonged exposure to light [S1].