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Postion:Product Catalog >SGI-7079
SGI-7079
  • SGI-7079

SGI-7079 NEW

Price $56 $98 $198
Package 5mg 10mg 25mg
Min. Order:
Supply Ability: 10g
Update Time: 2024-11-19

Product Details

Product Name: SGI-7079 CAS No.: 1239875-86-5
Purity: 99.26% Supply Ability: 10g
Release date: 2024/11/19

Product Introduction

Bioactivity

NameSGI-7079
DescriptionSGI-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 ResearchSGI-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 AssayIn 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 ResearchAnimal 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 vitroSGI-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 vivoSGI-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.
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility InformationEthanol : < 1 mg/mL (insoluble or slightly soluble)
DMSO : 84 mg/mL (184.4 mM)
H2O : < 1 mg/mL (insoluble or slightly soluble)
KeywordsTyro3 | inhibit | Inhibitor | Axl | Mer | TAM Receptor | SGI-7079 | SGI7079 | SGI 7079
Inhibitors RelatedGilteritinib | Nintedanib | Regorafenib monohydrate | Sorafenib | Staurosporine | L-Ascorbic acid 2-phosphate trisodium | Pexidartinib | Ibrutinib | Dasatinib | Regorafenib | Sorafenib tosylate | Lenvatinib mesylate
Related Compound LibrariesAnti-Lung 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 | Fluorochemical Library | Anti-Cancer Compound Library

Company Profile Introduction

Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers. TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.

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