产品描述:
CEP-40783 is an inhibitor of the receptor tyrosine kinases Axl and c-MET (IC50s = 7 and 12 nM, respectively).{43937} It inhibits Axl in 293GT cells expressing Axl and c-MET in NCI H1299 non-small cell lung cancer (NSCLC) cells with IC50 values of 0.26 and 6 nM, respectively. It also inhibits the receptor tyrosine kinases TYRO3 and MER (IC50s = 3.5 and 1.89 nM, respectively).{43938} CEP-40783 (0.3 mg/kg) induces complete regression of tumors in an Axl/NIH3T3 mouse xenograft model and reduces the metastatic tumor burden in mouse orthotopic breast cancer models. It also induces tumor stasis and regression in an EBC-1 NSCLC mouse xenograft model when administered at doses of 3 and 10 mg/kg, respectively. CEP-40783 reduces tumor growth in an MC38 mouse syngeneic model concomitantly with an increase in leukocyte infiltration into tumors, the production of IFN-γ in natural killer cells, and the percentage of CD8+ T cells in tumor tissue.{43938}