SGI-7079

Catalog No.S7847

SGI-7079 Chemical Structure

Molecular Weight(MW): 455.53

SGI-7079 ,a novel selective Axl inhibitor, inhibits tumor growth in a dose dependent manner and is a potential therapeutic target for overcoming EGFR inhibitor resistance.

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Biological Activity

Description SGI-7079 ,a novel selective Axl inhibitor, inhibits tumor growth in a dose dependent manner and is a potential therapeutic target for overcoming EGFR inhibitor resistance.
Targets
Met [1] Mer [1] YES [1] RET [1] FLT3 [1]
In vitro

SGI-7079 exhibits a Ki = 5.7 nM for AXL and inhibits Gas6 ligand-induced tyrosine phosphorylation of human AXL expressed in HEK293T cells (EC50 = 100 nM). It inhibits TAM family members MER and Tyro3 similarly as AXL, and shows potent, low nM inhibition of Syk, Flt1, Flt3, Jak2, TrkA, TrkB, PDGFRβ and Ret kinases. Mesenchymal cells express increased levels of the receptor tyrosine kinase Axl and show a trend toward greater sensitivity to the Axl inhibitor SGI-7079[2].

In vivo SGI-7079 inhibits tumor growth in a dose-dependent manner, and at the maximum dose, inhibits tumor growth by 67%, compared with control. the combination of SGI-7079 with erlotinib reverses erlotinib resistance in mesenchymal lines expressing Axl and in a xenograft model of mesenchymal NSCLC[2].

Protocol

Cell Research:

[2]

+ Expand
  • Cell lines: HEK-293 cells
  • Concentrations: 0.03, 0.1, 0.3, 1, 3 μmol/L
  • Incubation Time: 10 min
  • Method:

    To show inhibition of Axl activation by SGI-7079, HEK-293 cells are transiently transfected by electroporation with 1 mg FLAG-tagged plasmid containing the human Axl gene (OriGene Technologies) and allowed to incubate in standard media + 10% FBS for 24 hours. Cells are treated with SGI-7079 for 10 minutes at the indicated concentrations. Five minutes before lysis, the cells are stimulated with Gas6-containing WI38 conditioned media.


    (Only for Reference)
Animal Research:

[2]

+ Expand
  • Animal Models: Mouse(NCr-nu/nu female mice) xenograft model of NSCLC using the mesenchymal NSCLC cell line A549
  • Formulation: 0.1N citrate buffer
  • Dosages: 10, 25, 50 mg/kg
  • Administration: p.o.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 91 mg/mL (199.76 mM)
Water Insoluble
Ethanol 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 455.53
Formula

C26H26FN7

CAS No. 1239875-86-5
Storage powder
Synonyms N/A

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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

Tel: +1-832-582-8158 Ext:3

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID