Home Protein Tyrosine Kinase Axl inhibitor SGI-7079 For research use only.

SGI-7079

SGI-7079, a novel selective Axl inhibitor with an IC50 of 58 nM in vitro, inhibits tumor growth in a dose dependent manner and is a potential therapeutic target for overcoming EGFR inhibitor resistance.

SGI-7079 Chemical Structure

SGI-7079 Chemical Structure

CAS No. 1239875-86-5

Purity & Quality Control

Batch: S784701 DMSO]91 mg/mL]false]Water]Insoluble]false]Ethanol]Insoluble]false Purity: 99.68%
99.68

SGI-7079 Related Products

Biological Activity

Description SGI-7079, a novel selective Axl inhibitor with an IC50 of 58 nM in vitro, 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] Click to View More Targets
In vitro
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].
Cell Research 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 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.
In Vivo
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].
Animal Research Animal Models Mouse(NCr-nu/nu female mice) xenograft model of NSCLC using the mesenchymal NSCLC cell line A549
Dosages 10, 25, 50 mg/kg
Administration p.o.

Chemical Information & Solubility

Molecular Weight 455.53 Formula

C26H26FN7
CAS No. 1239875-86-5 SDF Download SGI-7079 SDF
Smiles CC1=CNC2=NC(=NC(=C12)C3=CC=CC(=C3)CC#N)NC4=CC(=C(C=C4)N5CCN(CC5)C)F
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 91 mg/mL ( (199.76 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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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

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