Home Protein Tyrosine Kinase c-Kit inhibitor - Ephrin receptor inhibitor - Axl inhibitor - VEGFR inhibitor - Trk receptor inhibitor Sitravatinib (MGCD516) For research use only.

Sitravatinib (MGCD516)

Synonyms: MG-516

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.

Sitravatinib (MGCD516) Chemical Structure

Sitravatinib (MGCD516) Chemical Structure

CAS No. 1123837-84-2

Purity & Quality Control

Sitravatinib (MGCD516) Related Products

Signaling Pathway

c-Kit Signaling Pathways

c-Kit Signaling Pathway

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
KB-8-5-11 qHTS assay P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen, Potency = 4.6109 μM. 31515284
KB-3-1 qHTS assay P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen 31515284
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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.
Targets
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)		 Click to View More Targets
0.5 nM 1 nM 1.5 nM 2 nM 2 nM
In vitro
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 Research 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
Experimental Result Images Methods Biomarkers Images PMID
Growth inhibition assay Cell viability 26675259
Western blot p-IGF1-R / IGF1-R / p-PDGFRβ / PDGFRβ/ p-AKT / AKT 26675259
In Vivo
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[2].
Animal Research Animal Models ICR/SCID mice
Dosages 15 mg/kg
Administration p.o.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT04935112 Completed
Healthy Adults
Mirati Therapeutics Inc.
 July 7 2021 Phase 1
NCT04921358 Terminated
Non-Small Cell Lung Cancer (NSCLC)
BeiGene
 July 27 2021 Phase 3
NCT04772612 Completed
Hepatic Impairment
Mirati Therapeutics Inc.
 March 12 2021 Phase 1
NCT04800614 Completed
Healthy Adults
Mirati Therapeutics Inc.
 March 15 2021 Phase 1

Chemical Information & Solubility

Molecular Weight 629.68 Formula

C33H29F2N5O4S
CAS No. 1123837-84-2 SDF Download Sitravatinib (MGCD516) SDF
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
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 100 mg/mL ( (158.81 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 100 mg/mL

Water : Insoluble


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In vivo
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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.

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