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Catalog No. T4349   CAS 1123837-84-2
Synonyms: MG516, MGCD516

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

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Sitravatinib, CAS 1123837-84-2
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Purity: 98%
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Biological Description
Chemical Properties
Storage & Solubility Information
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.
Targets&IC50 DDR2:0.5 nM, EPHA3:1 nM, Mer:2 nM, VEGFR3 (FLT4):2 nM, Axl:1.5 nM
In vitro MGCD516 (Sitravatinib) 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. MGCD516 causes the marked blockade of phosphorylation of potential driver RTKs and induced potent anti-proliferative effects in vitro.
In vivo Sitravatinib 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.
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.
Synonyms MG516, MGCD516
Molecular Weight 629.68
Formula C33H29F2N5O4S
CAS No. 1123837-84-2


Powder: -20°C for 3 years

In solvent: -80°C for 2 years

Solubility Information

DMSO: 32 mg/mL

( < 1 mg/ml refers to the product slightly soluble or insoluble )

References and Literature

1. Patwardhan PP et al. Significant blockade of multiple receptor tyrosine kinases by MGCD516 (Sitravatinib), a novel small molecule inhibitor, shows potent anti-tumor activity in preClinicalal models of sarcoma. Oncotarget, 2016 Jan 26;7(4):4093-109.

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Sitravatinib 1123837-84-2 Angiogenesis Tyrosine Kinase/Adaptors Trk receptor FLT TAM Receptor Discoidin Domain Receptor (DDR) VEGFR Ephrin Receptor c-Kit RTK MG-516 PD-1 SCFR DDR1 inhibit VEGFR2 MG 516 MGCD 516 MER immune MG516 TRKA Cluster of differentiation antigen 135 Cancer Discoidin Domain Receptor VEGFR3 Inhibitor Vascular endothelial growth factor receptor Trk Receptor Tropomyosin related kinase receptor CD135 MGCD516 immunotherapy Macrophages DDR2 VEGFR1 Tyrosine Fms like tyrosine kinase 3 FLT3 Axl TRKB MGCD-516 KIT kinase CD117 inhibitor