Sitravatinib (MGCD516)

For research use only.

Catalog No.S8573 Synonyms: MG-516

1 publication

Sitravatinib (MGCD516) Chemical Structure

CAS No. 1123837-84-2

Sitravatinib (MGCD516, MG-516) is a novel small molecule inhibitor targeting multiple RTKs involved in driving sarcoma cell growth, including c-Kit, PDGFRβ, PDGFRα, c-Met, and Axl.

Selleck's Sitravatinib (MGCD516) has been cited by 1 publication

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Biological Activity

Description Sitravatinib (MGCD516, MG-516) is a novel small molecule inhibitor targeting multiple RTKs involved in driving sarcoma cell growth, including c-Kit, PDGFRβ, PDGFRα, c-Met, and Axl.
DDR2 [2]
(Cell-free assay)
EPHA3 [2]
(Cell-free assay)
Axl [2]
(Cell-free assay)
Mer [2]
(Cell-free assay)
VEGFR3 (FLT4) [2]
(Cell-free assay)
0.5 nM 1 nM 1.5 nM 2 nM 2 nM
In vitro

MGCD516 (Sitravatinib), is an oral, potent small molecule inhibitor of a closely related spectrum of RTKs including RET, the split RTKs (VEGFR, PDGFR and KIT), TRK family, DDR2, MET and AXL[1]. MGCD516 treatment resulted in significant blockade of phosphorylation of potential driver RTKs and induced potent anti-proliferative effects in vitro[2].

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
KB-8-5-11 MVPxTHRUKGG|c3H5 NFjMb29RNWeueXPvdJJwfGWrbjDzeYJ{fHKjdHXzJIll\W62aX\p[YQhcW5iS1KtPE02NTFzIHHk[Y5w[2G{Y3nuc41iKGOnbHygcIlv\SxicVjUV{B1cGW{YYDleZRq[yCuaXLyZZJ6KHOlcnXlckwhWG:2ZX7jfUA:KDRwNkGwPUDPxE1w NFrrPW49[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MUWxOVI5PCd-M{G1NVUzQDR:L3G+
KB-3-1 NFficJFyUFSVIHHzd4F6 M{L0dnAu\2y7Y3;wdo91\WmwIIP1ZpN1emG2ZYOgbYRmdnSrZnnl[EBqdiCNQj2zMVEh[WSnbn;jZZJkcW6xbXGgZ4VtdCCuaX7lMEByUFSVIITo[ZJieGW3dHnjJIxq[nKjcomgd4Nz\WWw NUXMfJY6RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{G1NVUzQDRpPkOxOVE2Ojh2PD;hQi=>

... Click to View More Cell Line Experimental Data

Methods Test Index PMID
Growth inhibition assay
Cell viability; 

PubMed: 26675259     

Indicated cell lines were plated in 96-well plates and treated in six wells per condition with increasing doses of MGCD516 for 72 hours. Cell viability was measured using Dojindo Cell Counting Kit 8. Dose response graphs were generated as a percentage of the no drug control. Error bars represent standard error mean. Combined data from three independent experiments is shown. 

Western blot
p-IGF1-R / IGF1-R / p-PDGFRβ / PDGFRβ/ p-AKT / AKT ; 

PubMed: 26675259     

Indicated cell lines were grown to 60% confluency in serum free media overnight. Next day, cells were treated with indicated concentrations of MGCD516 in serum free media for 3 hours. After the drug treatments, cells were stimulated in drug free media containing 10%FBS. Media containing no FBS was used as unstimulated control. 20 to 30 micrograms of RIPA lysates were loaded on SDS/PAGE and immunoblotted using indicated antibodies. Representative western blots from two independent experiments are shown. ND=No Drug, Uns=Unstimulated control.

In vivo Sitravatinib has demonstrated antitumor activity in nonclinical cancer models harboring genetic alterations of sitravatinib targets, including rearrangement of RET, NTRK, or CHR4q12 amplification[1]. MGCD516 treatment of tumor xenografts in vivo resulted in significant suppression of tumor growth. Efficacy of MGCD516 was superior to imatinib and crizotinib, two other well-studied multi-kinase inhibitors with overlapping target specificities, both in vitro and in vivo[2].


Cell Research:


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  • Cell lines: DDLS, LS141 and MPNST
  • Concentrations: 62.5, 125, 250, 500, 1000, 2000 nM/L
  • Incubation Time: 72 h
  • Method:

    2,000-3,000 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. IC50 was extrapolated from cell viability data using CompuSyn software according to the manufacturer's instructions

    (Only for Reference)
Animal Research:


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  • Animal Models: ICR/SCID mice
  • Dosages: 15 mg/kg
  • Administration: p.o.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 100 mg/mL (158.81 mM)
Water Insoluble
Ethanol '100 mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 629.68


CAS No. 1123837-84-2
Storage powder
in solvent
Synonyms MG-516
Smiles COCCNCC1=CN=C(C=C1)C2=CC3=NC=CC(=C3S2)OC4=C(C=C(C=C4)NC(=O)C5(CC5)C(=O)NC6=CC=C(C=C6)F)F

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04935112 Not yet recruiting Drug: Sitravatinib|Drug: Pantoprazole|Drug: Famotidine Healthy Adults Mirati Therapeutics Inc. July 2021 Phase 1
NCT04800614 Active not recruiting Drug: sitravatinib Healthy Adults Mirati Therapeutics Inc. March 15 2021 Phase 1
NCT04772612 Recruiting Drug: sitravatinib Hepatic Impairment Mirati Therapeutics Inc. March 12 2021 Phase 1
NCT03680521 Active not recruiting Drug: Sitravatinib|Drug: Nivolumab Clear Cell Renal Cell Carcinoma Mirati Therapeutics Inc. October 10 2018 Phase 2

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c-Kit Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID