| Name | SGI-7079 |
| Description | SGI-7079 is a new selective Axl inhibitor. SGI-7079 can be a dose-dependent manner inhibited growth of tumors. It is also a potential therapeutic target for EGFR inhibitor resistance. |
| Cell Research | SGI-7079 show inhibition of Axl activation in HEK-293 cells, which were transiently transfected by electroporation with 1 mg FLAG-tagged plasmid containing the human Axl gene and incubated in standard media + 10% FBS for 24 hours.Cells are treated with SGI-7079( concentrations : 0.03, 0.1, 0.3, 1, 3 μmol/L) for 10 minutes. Five minutes before lysis, the cells are stimulated by WI38 conditioned media containing Gas6. |
| Kinase Assay | In phospho-GEF-H1 cellular assay, TR-293-KDG cells are incubated for 3 hours with PF-3758309. TR-293-KDG cells were captured on an anti-HA antibody-coated plate, which is detected with an anti-phospho-S810-GEF-H1 antibody, and quantified with a horseradish peroxidase-goat anti-rabbit antibody conjugate. TR-293-KDG cells are constructed from HEK293 cells, which is transfected with tetracycline-inducible PAK4-kinase domain (amino acids 291-591) and expressed HA-tagged GEFH1ΔDH (amino acids 210-921). |
| Animal Research | Animal Models: Mouse(NCr-nu/nu female mice) xenograft model of NSCLC using the mesenchymal NSCLC cell line A549Formulation: 0.1N citrate bufferDosages: 10, 25, 50 mg/kgAdministration: p.o. |
| In vitro | SGI-7079 exhibits a Ki = 5.7 nM for AXL ,and in HEK293T cells (EC50 = 100 nM) inhibits Gas6 ligand-induced tyrosine phosphorylation of human AXL expressed . Similar to AXL, SGI-7079 inhibits TAM family members such as MER and Tyro3, and shows effective inhibition of Syk, Flt1, Flt3, Jak2, TrkA, TrkB, PDGFRβ and Ret kinases. Mesenchymal cells, which have the increase of the receptor tyrosine kinase Axl, show a trend that has greater sensitivity to the Axl inhibitor SGI-7079. |
| In vivo | SGI-7079 can be in a dose-dependent manner inhibits tumor growth. And at the maximum dose, 67% tumor can be inhibited growth. Mesenchymal cells showed a trend towards a greater sensitivity to the Axl inhibitor SGI-7079, while the combination of SGI-7079 with erlotinib reversed erlotinib resistance in mesenchymal lines expressing Axl and in a xenograft model of mesenchymal NSCLC. |
| Storage | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | Ethanol : < 1 mg/mL (insoluble or slightly soluble)
10% DMSO+40% PEG300+5% Tween 80+45% Saline : 3.3 mg/mL (7.24 mM), Sonication is recommended.
DMSO : 250 mg/mL (548.81 mM), Sonication is recommended.
H2O : < 1 mg/mL (insoluble or slightly soluble)
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| Keywords | Yes | Tyro3 | TAMReceptor | TAM Receptor | SGI-7079 | SGI7079 | SGI 7079 | RET | Met | Mer | Inhibitor | inhibit | HGFR | FLT3 | cRET | cMet/HGFR | c-Met | cMet | Axl |
| Inhibitors Related | Bemcentinib | Gilteritinib | Decanoic Acid | Sorafenib | Dasatinib | Ibrutinib | Pexidartinib | Regorafenib | Afatinib | Brigatinib | Bacitracin Zinc | Lenvatinib |
| Related Compound Libraries | Apoptosis Compound Library | Anti-Colorectal Cancer Compound Library | Anti-Pancreatic Cancer Compound Library | Bioactive Compound Library | Membrane Protein-targeted Compound Library | HIF-1 Signaling Pathway Compound Library | Kinase Inhibitor Library | Tyrosine Kinase Inhibitor Library | Inhibitor Library | Bioactive Compounds Library Max | Anti-Cancer Compound Library | Anti-Liver Cancer Compound Library |
United States
