Lapatinib ditosylate

Lapatinib is a synthetic, orally-active quinazoline with potential antineoplastic activity. Lapatinib reversibly blocks phosphorylation of the epidermal growth factor receptor (EGFR), ErbB2, and the Erk-1 and-2 and AKT kinases; it also inhibits cyclin D protein levels in human tumor cell lines and xenografts. EGFR and ErbB2 have been implicated in the growth of various tumor types. Check for active clinical trials or closed clinical trials using this agent.

Lapatinib (GW-572016) Ditosylate is a potent EGFR and ErbB2 inhibitor with IC50 of 10.8 and 9.2 nM in cell-free assays, respectively.

Properties:

Appearance & Physical State: Yellow solid

Boiling Point: 750.7ºC at 760 mmHg

Melting Point: 240-242ºC

Flash Point: 407.8ºC

HER2 Inhibitors Related Products:

[1]. Rusnak DW, et al. 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. Mol Cancer Ther. 2001 Dec;1(2):85-94.

[2]. O'Neill F, et al. Gene expression changes as markers of early lapatinib response in a panel of breast cancer cell lines. Mol Cancer. 2012 Jun 18;11(1):41.

[3]. Eryilmaz U, et al. S100A1 as a Potential Diagnostic Biomarker for Assessing Cardiotoxicity and Implications for the Chemotherapy of Certain Cancers. PLoS One. 2015 Dec 18;10(12):e0145418.