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Sitravatinib (MGCD516) c-Kit inhibitor

Name: Sitravatinib (MGCD516)
Brand: Selleck Chemicals
SKU: S8573
Availability: InStock
Rating: 5 (6 reviews)

Cat.No.S8573

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.

Chemical Structure

Molecular Weight: 629.68

Jump to Mechanism of Action Cell Culture & Working Concentration Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: Purity: 99.97%

99.97

Related Targets	EGFR VEGFR PDGFR FGFR c-Met Src FLT3 HER2 Bcr-Abl MEK BTK IGF-1R ALK Trk receptor Syk Axl CSF-1R c-RET FAK Mertk Tie-2 DYRK Tyro3 Ephrin receptor ROS1 Pyk2 RON DDR ACK Fer kinase
Related Products	Masitinib Amuvatinib (MP-470) OSI-930 ISCK03 PDGFR inhibitor 1 Elenestinib phosphate M4205（IDRX-42） Masitinib mesylate AZD3229 Bezuclastinib c-Kit Antibody [C9J3]

Cell Culture, Treatment & Working Concentration

Cell Lines	Assay Type	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
Click to View More Cell Line Experimental Data

Chemical Information, Storage & Stability

Molecular Weight	629.68	Formula	C₃₃H₂₉F₂N₅O₄S	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	1123837-84-2	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin 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

Solubility

In vitro
Batch:

DMSO : 100 mg/mL (158.81 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 100 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	5.000mg/ml (7.94mM)	Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.830mg/ml (1.32mM)	Taking the 1 mL working solution as an example, add 50 μL of 16.6 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

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:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC₅₀/Ki	DDR2 ^[2] (Cell-free assay) 0.5 nM EPHA3 ^[2] (Cell-free assay) 1 nM Axl ^[2] (Cell-free assay) 1.5 nM Mer ^[2] (Cell-free assay) 2 nM VEGFR3 (FLT4) ^[2] (Cell-free assay) 2 nM VEGFR2 (KDR) ^[2] (Cell-free assay) 5 nM TRKA (NTRK1) ^[2] (Cell-free assay) 5 nM VEGFR1 (FLT1) ^[2] (Cell-free assay) 6 nM Kit ^[2] (Cell-free assay) 6 nM FLT3 ^[2] (Cell-free assay) 8 nM TRKB (NTRK2) ^[2] (Cell-free assay) 9 nM EPHB2 ^[2] (Cell-free assay) 10 nM EPHB4 ^[2] (Cell-free assay) 12 nM Met ^[2] (Cell-free assay) 20 nM DDR1 ^[2] (Cell-free assay) 29 nM PDGFRα ^[2] (Cell-free assay) 30 nM RON ^[2] (Cell-free assay) 43 nM RET ^[2] (Cell-free assay) 44 nM EphA2 ^[2] (Cell-free assay) 44 nM ROS ^[2] (Cell-free assay) 59 nM EPHA4 ^[2] (Cell-free assay) 76 nM Src ^[2] (Cell-free assay) 156 nM
In vitro	Sitravatinib (MGCD516) 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]. Treatment with this compound resulted in significant blockade of phosphorylation of potential driver RTKs and induced potent anti-proliferative effects in vitro^[2].
In vivo	Sitravatinib (MGCD516) has demonstrated antitumor activity in nonclinical cancer models harboring genetic alterations of its targets, including rearrangement of RET, NTRK, or CHR4q12 amplification^[1]. Treatment of tumor xenografts in vivo with this compound resulted in significant suppression of tumor growth^[2].
References	[1] http://www.jto.org/article/S1556-0864(16)32735-6/pdf [2] https://pubmed.ncbi.nlm.nih.gov/26675259/

Applications

Methods	Biomarkers	Images	PMID
Growth inhibition assay	Cell viability		26675259
Western blot	p-IGF1-R / IGF1-R / p-PDGFRβ / PDGFRβ/ p-AKT / AKT		26675259

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

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

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