CAS: 1268997-70-1

O-De(3-fluorobenzyl) lapatinib (OFL) is a tyrosine kinase inhibitor that inhibits epidermal growth factor receptor, b-raf, and epidermal growth factor. It also inhibits the serine/threonine protein kinase activity of lapatinib, which is found in the cells of breast cancer. OFL has been shown to inhibit tumor growth in vitro studies. The drug was able to decrease the levels of reactive oxygen species (ROS) in cells by up to 50%. In addition, it may have anti-inflammatory properties due to its ability to inhibit the production of cytokines such as IL-6, TNF-α, and IL-8.

Applications A reactive metabolite of Lapatinib (L175800) which is associated with various drug toxicities. Lapatinib is metabolized mainly by P450 3A4 to form O- and N-dealkylated metabolites. References He, K., et al.: Chem. Res. Toxicol., 11, 252 (1998), Rusnuk, D., et al.: Cancer Res., 61, 7196 (2001), Li, X., et al.: Drug Metab. Dispos., 37, 1242 (2009),