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.

Size Price Stock Quantity  
10mM (1mL in DMSO) USD 207 In stock
USD 97 In stock
USD 247 In stock
USD 527 In stock
Bulk Discount

Free Overnight Delivery on orders over $ 500
Next day delivery by 10:00 a.m. Order now.

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

Purity & Quality Control

Choose Selective c-Kit Inhibitors

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].

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:


- Collapse
  • 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:


- Collapse
  • 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

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
Dosage mg/kg Average weight of animals g Dosing volume per animal ul Number of animals
Step 2: Enter the in vivo formulation ()
% DMSO % % Tween 80 % ddH2O

Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

  • Mass
    Molecular Weight

*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

  • C1

* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

  • Serial Dilutions

  • Computed Result

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

  • * Indicates a Required Field

c-Kit Signaling Pathway Map

Related c-Kit Products

Tags: buy Sitravatinib (MGCD516) | Sitravatinib (MGCD516) supplier | purchase Sitravatinib (MGCD516) | Sitravatinib (MGCD516) cost | Sitravatinib (MGCD516) manufacturer | order Sitravatinib (MGCD516) | Sitravatinib (MGCD516) distributor
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID