XL092 is an orally active, ATP-competitive inhibitor of multiple receptor tyrosine kinases (RTKs) including MET, VEGFR2, AXL and MER, with IC50s in cell-based assays of 15 nM, 1.6 nM, 3.4 nM, 7.2 nM respectively. XL092 exhibits anti-tumor activity. XL092 has the potential for kinase-dependent diseases and conditions research[2].In Vivo: XL092 (10 mg/kg/day; oral; for 14 days) causes substantial tumor growth inhibition in xenograft studies. XL092 shows 82% and 96% inhibition on p-MET and p-VEGFR2, respectively.
XL092 (compound 8; 3 mg/kg; iv) has a T1/2 of 5.4 hours, a CL of 43 mL/hr?kg. XL092 (3 mg/kg; po) has a T1/2 of 7.1 hours and a Cmax of 11.4 μM for rats[2].