Sitravatinib (MGCD516) is an inhibitor targeting multiple RTKs involved in driving sarcoma cell growth, including c-Met, c-Kit, PDGFRα/β, PDGFR, and Axl.

TrkA:5 nM, VEGFR2:5 nM, FLT3:8 nM, Axl:1.5 nM, VEGFR3/FLT4:2 nM, Mer:2 nM, DDR2:0.5 nM, TrkB:9 nM, VEGFR1:6 nM, DDR1:29 nM, c-Kit:6 nM, EphA3:1 nM

Cell lines: DDLS,LS141,and MPNST. Concentrations: 62.5,125,250,500,1000,2000 nM2,000-3,000 cells were plated in 96-well plates in RPMI/DME media with 10% FBS and then treated with the indicated drugs the next day.After 72 hours,media was replaced with 100 μL of media with 10% serum and 10% CCK-8 solution.After 1 hour,the optical density was read at 450 nm to determine viability.Background values from negative control wells without cells were subtracted for final sample quantification.Data was plotted as % cell viability compared to DMSO control.

Animal Models: ICR/SCID mice. Formulation: 0.5% hydroxypropyl methylcellulose (HPMC) and 0.1% Tween-80 solution (pH 1.4). Dosages: 15 mg/kg. Administration: p.o.