产品描述:
The hepatocyte growth factor receptor c-Met commonly shows elevated activity in several forms of cancer.{29341,29344} SGX523 is a potent, selective, ATP-competitive inhibitor that blocks the tyrosine kinase activity of c-Met with an IC50 value of 4 nM.{29341} It is over 1,000-fold selective for c-Met over a panel of other kinases.{29341} SGX523 is orally active and dose-dependently inhibits the growth of a variety of tumor xenografts in mice.{29341,29343} The effectiveness of SGX523 is enhanced when combined with other chemotherapeutic compounds, including inhibitors of EGFR.{29344,29345} SGX523 is metabolized, at least in part, by aldehyde oxidase, an enzyme that differs in activity across different species.{29342}