Sitravatinib (MGCD516)

Catalog No.S8573 Batch:S857303

Technical Data

Formula	C₃₃H₂₉F₂N₅O₄S
Molecular Weight	629.68	CAS No.	1123837-84-2
Solubility (25°C)*	In vitro	DMSO	100 mg/mL (158.81 mM)
		Ethanol	5 mg/mL (7.94 mM)
		Water	Insoluble
* <1 mg/ml means slightly soluble or insoluble. * 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. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

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)	View More
0.5 nM	1 nM	1.5 nM	2 nM	2 nM	View More

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].

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 Assay:^{^[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 Study:^{^[2]}	Animal Models ICR/SCID mice Dosages 15 mg/kg Administration p.o.

Cell Assay:^{^[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 Study:^{^[2]}

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

References

Selleck's Sitravatinib (MGCD516) has been cited by 3 publications

An in vivo model of glioblastoma radiation resistance identifies long non-coding RNAs and targetable kinases [ JCI Insight, 2022, e148717]	PubMed: 35852875
SMARCA4 Depletion Induces Cisplatin Resistance by Activating YAP1-Mediated Epithelial-to-Mesenchymal Transition in Triple-Negative Breast Cancer [ Cancers (Basel), 2021, 13(21)5474]	PubMed: 34771636
Sitravatinib Sensitizes ABCB1- and ABCG2-Overexpressing Multidrug-Resistant Cancer Cells to Chemotherapeutic Drugs. [ Cancers (Basel), 2020, 12(1)]	PubMed: 31941029

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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