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Sitravatinib

Catalog No. T4349 CAS 1123837-84-2

Synonyms: MG516, MGCD516

Sitravatinib (MGCD516) is an inhibitor targeting multiple RTKs involved in driving sarcoma cell growth, including c-Met, c-Kit, PDGFRα/β, PDGFR, and Axl.

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Sitravatinib, CAS 1123837-84-2

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Purity: 98%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	Sitravatinib (MGCD516) is an inhibitor targeting multiple RTKs involved in driving sarcoma cell growth, including c-Met, c-Kit, PDGFRα/β, PDGFR, and Axl.
Targets&IC50	DDR2:0.5 nM, EPHA3:1 nM, Mer:2 nM, VEGFR3 (FLT4):2 nM, Axl:1.5 nM
In vitro	MGCD516 (Sitravatinib) is an inhibitor of a closely related spectrum of RTKs including RET, the split RTKs (PDGFR, VEGFR, and KIT), DDR2, TRK family, MET, and AXL. MGCD516 causes the marked blockade of phosphorylation of potential driver RTKs and induced potent anti-proliferative effects in vitro.
In vivo	Sitravatinib has antitumor activity in nonClinicalal cancer models harboring genetic alterations of sitravatinib targets, including the rearrangement of NTRK, RET, or CHR4q12 amplification. In vivo tumor xenografts, MGCD516 causes the significant suppression of tumor growth. Efficacy of MGCD516 is superior to imatinib and crizotinib, two other well-studied multi-kinase inhibitors with overlapping target specificities, both in vitro and in vivo.
Cell Research	Cell lines: DDLS,LS141,and MPNST. Concentrations: 62.5,125,250,500,1000,2000 nM2,000-3,000 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.
Animal Research	Animal Models: ICR/SCID mice. Formulation: 0.5% hydroxypropyl methylcellulose (HPMC) and 0.1% Tween-80 solution (pH 1.4). Dosages: 15 mg/kg. Administration: p.o.

Synonyms	MG516, MGCD516
Molecular Weight	629.68
Formula	C33H29F2N5O4S
CAS No.	1123837-84-2

Storage

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

Solubility Information

DMSO: 32 mg/mL

( < 1 mg/ml refers to the product slightly soluble or insoluble )

References and Literature

1. Patwardhan PP et al. Significant blockade of multiple receptor tyrosine kinases by MGCD516 (Sitravatinib), a novel small molecule inhibitor, shows potent anti-tumor activity in preClinicalal models of sarcoma. Oncotarget, 2016 Jan 26;7(4):4093-109.

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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 add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

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Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

Sitravatinib 1123837-84-2 Angiogenesis Tyrosine Kinase/Adaptors Trk receptor FLT TAM Receptor Discoidin Domain Receptor (DDR) VEGFR Ephrin Receptor c-Kit RTK MG-516 PD-1 SCFR DDR1 inhibit VEGFR2 MG 516 MGCD 516 MER immune MG516 TRKA Cluster of differentiation antigen 135 Cancer Discoidin Domain Receptor VEGFR3 Inhibitor Vascular endothelial growth factor receptor Trk Receptor Tropomyosin related kinase receptor CD135 MGCD516 immunotherapy Macrophages DDR2 VEGFR1 Tyrosine Fms like tyrosine kinase 3 FLT3 Axl TRKB MGCD-516 KIT kinase CD117 inhibitor

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