Sitravatinib (MGCD516)

Catalog No.S8573 Synonyms: MG-516

Sitravatinib (MGCD516) Chemical Structure

Molecular Weight(MW): 629.68

Sitravatinib (MGCD516) is a novel small molecule inhibitor targeting multiple RTKs involved in driving sarcoma cell growth, including c-Kit, PDGFRβ, PDGFRα, c-Met, and Axl.

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Biological Activity

Description Sitravatinib (MGCD516) 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)
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].

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

Cell Research:

[2]

+ Expand
  • 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


    (Only for Reference)
Animal Research:

[2]

+ Expand
  • 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.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 100 mg/mL (158.81 mM)
Ethanol 100 mg/mL (158.81 mM)
Water 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.

Chemical Information

Molecular Weight 629.68
Formula

C33H29F2N5O4S

CAS No. 1123837-84-2
Storage powder
Synonyms MG-516

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Related Antibodies

c-Kit Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID