Sitravatinib (MGCD516)

Catalog No.S8573 Synonyms: MG-516

For research use only.

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

CAS No. 1123837-84-2

Selleck's Sitravatinib (MGCD516) has been cited by 2 Publications

Purity & Quality Control

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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

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 NYjab3VyeUiWUzDhd5NigQ>? MYXQMYdtgWOxcILveIVqdiC|dXLzeJJifGW|IHnk[Y51cW[rZXSgbY4hU0JvOD21MVEyKGGmZX7vZ4Fz[2mwb33hJINmdGxibHnu[UwheUiWUzD0bIVz[XCndYTpZ{BtcWK{YYL5JJNkemWnbjygVI91\W6leTC9JFQvPjFyOTFOwG0v MoPoQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzF3MUWyPFQoRjNzNUG1Nlg1RC:jPh?=
KB-3-1 MnzEdWhVWyCjc4PhfS=> NIHW[ZVRNWeueXPvdJJwfGWrbjDzeYJ{fHKjdHXzJIll\W62aX\p[YQhcW5iS1KtN{0yKGGmZX7vZ4Fz[2mwb33hJINmdGxibHnu[UwheUiWUzD0bIVz[XCndYTpZ{BtcWK{YYL5JJNkemWnbh?= Mk\hQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzF3MUWyPFQoRjNzNUG1Nlg1RC:jPh?=
Assay
Methods Test Index PMID
Growth inhibition assay Cell viability 26675259
Western blot p-IGF1-R / IGF1-R / p-PDGFRβ / PDGFRβ/ p-AKT / AKT 26675259
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].

Protocol (from reference)

Cell Research:

[2]

  • 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

Animal Research:

[2]

  • Animal Models: ICR/SCID mice
  • Dosages: 15 mg/kg
  • Administration: p.o.

Solubility (25°C)

In vitro

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

Chemical Information

Molecular Weight 629.68
Formula

C33H29F2N5O4S

CAS No. 1123837-84-2
Storage 3 years -20°C powder
2 years -80°C in solvent
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)

mg/kg g μL

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.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04935112 Active not recruiting Drug: Sitravatinib|Drug: Pantoprazole|Drug: Famotidine Healthy Adults Mirati Therapeutics Inc. July 7 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
NCT04472650 Completed Drug: Sitravatinib Tumor BeiGene July 23 2020 Phase 1
NCT03680521 Active not recruiting Drug: Sitravatinib|Drug: Nivolumab Clear Cell Renal Cell Carcinoma Mirati Therapeutics Inc. October 10 2018 Phase 2

(data from https://clinicaltrials.gov, updated on 2022-01-17)

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

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