| Name | Sitravatinib |
| Description | Sitravatinib (MGCD516) is an inhibitor targeting multiple RTKs involved in driving sarcoma cell growth, including c-Met, c-Kit, PDGFRα/β, PDGFR, and Axl. |
| Cell Research | 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 Research | 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. |
| In vitro | Sitravatinib (MGCD516) is an inhibitor of a closely related spectrum of RTKs including RET, the split RTKs (PDGFR, VEGFR, and KIT), DDR2, TRK family, MET, and AXL. Sitravatinib causes the marked blockade of phosphorylation of potential driver RTKs and induced potent anti-proliferative effects in vitro. |
| In vivo | Sitravatinib (MGCD516) has antitumor activity in nonClinicalal cancer models harboring genetic alterations of sitravatinib targets, including the rearrangement of NTRK, RET, or CHR4q12 amplification. In vivo tumor xenografts, MGCD516 causes the significant suppression of tumor growth. Efficacy of MGCD516 is superior to imatinib and crizotinib, two other well-studied multi-kinase inhibitors with overlapping target specificities, both in vitro and in vivo. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | 10% DMSO+90% Corn Oil : 2.5 mg/mL (3.97 mM), Sonication is recommended.
DMSO : 250 mg/mL (397.03 mM), Sonication is recommended.
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| Keywords | VEGFR3/FLT4 | VEGFR3 | VEGFR2 | VEGFR1 | VEGFR | Vascular endothelial growth factor receptor | Tyrosine | Tropomyosin related kinase receptor | Trkreceptor | TRKB | TRKA | Trk receptor | TAMReceptor | TAM Receptor | Sitravatinib | SCFR | RTK | PD-1 | MGCD-516 | MGCD 516 | MG-516 | MG 516 | MER | Macrophages | KIT | kinase | Inhibitor | inhibit | immunotherapy | immune | Fms like tyrosine kinase 3 | FLT3 | EphrinReceptor | Ephrin Receptor | EphA3 | DiscoidinDomainReceptor(DDR) | DiscoidinDomainReceptor | Discoidin Domain Receptor (DDR) | Discoidin Domain Receptor | DDR2 | DDR1 | DDR | Cluster of differentiation antigen 135 | c-Kit | cKit | CD135 | CD117 | Cancer | Axl |
| Inhibitors Related | Ribociclib | Bemcentinib | Gilteritinib | Sorafenib | Dasatinib | Pexidartinib | glycine | Nintedanib esylate | Chloramphenicol | Lenvatinib | NSI-189 Phosphate | Pazopanib |
| Related Compound Libraries | Failed Clinical Trials Compound Library | Bioactive Compound Library | Membrane Protein-targeted Compound Library | Kinase Inhibitor Library | Tyrosine Kinase Inhibitor Library | Anti-Cancer Clinical Compound Library | Drug Repurposing Compound Library | Inhibitor Library | Immunology/Inflammation Compound Library | Bioactive Compounds Library Max | Anti-Cancer Drug Library | Anti-Cancer Active Compound Library |
United States
