SGI-7079

Catalog No.S7847 Batch:S784701

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Technical Data

Formula

C26H26FN7

Molecular Weight 455.53 CAS No. 1239875-86-5
Solubility (25°C)* In vitro DMSO 91 mg/mL (199.76 mM)
Water Insoluble
Ethanol 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.)

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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] View More
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 (from reference)

Cell Assay:

[2]

  • 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.

Animal Study:

[2]

  • 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.

Customer Product Validation

Data from [Data independently produced by , , Oncotarget, 2017, 8(52): 89761–89774 ]

Selleck's SGI-7079 has been cited by 3 publications

SIRT3 overexpression and epigenetic silencing of catalase regulate ROS accumulation in CLL cells activating AXL signaling axis [ Blood Cancer J, 2021, 11(5):93] PubMed: 34001853
Integrative Analysis Identifies a Novel AXL-PI3 Kinase-PD-L1 Signaling Axis Associated with Radiation Resistance in Head and Neck Cancer [ Clin Cancer Res, 2017, 23(11):2713-2722] PubMed: 28476872
Axl inhibition induces the antitumor immune response which can be further potentiated by PD-1 blockade in the mouse cancer models. [ Oncotarget, 2017, 8(52):89761-89774] PubMed: 29163786

RETURN POLICY
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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.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.