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SGI-7079

SGI-7079
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Purity:99.26%
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SGI-7079

Catalog No. T6982Cas No. 1239875-86-5
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.
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Pack SizePriceAvailabilityQuantity
2 mg$35In Stock
5 mg$56In Stock
10 mg$98In Stock
25 mg$198In Stock
50 mg$255In Stock
100 mg$372In Stock
500 mg$869In Stock
1 mL x 10 mM (in DMSO)$62In Stock
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Product Introduction

Bioactivity
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.
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.
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).
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.
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.
Chemical Properties
Molecular Weight455.53
FormulaC26H26FN7
Cas No.1239875-86-5
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year
Solubility Information
Ethanol: < 1 mg/mL (insoluble or slightly soluble)
DMSO: 84 mg/mL (184.4 mM)
H2O: < 1 mg/mL (insoluble or slightly soluble)
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM2.1952 mL10.9762 mL21.9525 mL109.7623 mL
5 mM0.4390 mL2.1952 mL4.3905 mL21.9525 mL
10 mM0.2195 mL1.0976 mL2.1952 mL10.9762 mL
20 mM0.1098 mL0.5488 mL1.0976 mL5.4881 mL
50 mM0.0439 mL0.2195 mL0.4390 mL2.1952 mL
100 mM0.0220 mL0.1098 mL0.2195 mL1.0976 mL

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