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SGI-7079

Catalog No. T6982   CAS 1239875-86-5
Synonyms: SGI7079, SGI 7079

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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SGI-7079, CAS 1239875-86-5
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Purity: 98%
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Biological Description
Chemical Properties
Storage & Solubility Information
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.
Synonyms SGI7079, SGI 7079
Molecular Weight 455.541
Formula C26H26FN7
CAS No. 1239875-86-5

Storage

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

Solubility Information

Ethanol: <1 mg/mL

DMSO: 84 mg/mL (184.4 mM)

H2O: <1 mg/mL

( < 1 mg/ml refers to the product slightly soluble or insoluble )

References and Literature

1. Myers SH, et al. J Med Chem. 2016, 59(8):3593-608. 2. Byers LA, et al. Clin Cancer Res. 2013, 19(1):279-90.

Related compound libraries

This product is contained In the following compound libraries:
Anti-Cancer Compound Library Anti-Lung Cancer Compound Library HIF-1 Signaling Pathway Compound Library Anti-Obesity Compound Library Inhibitor Library Fluorochemical Library Anti-Cancer Active Compound Library Kinase Inhibitor Library Apoptosis Compound Library Angiogenesis related Compound Library

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Keywords

SGI-7079 1239875-86-5 蛋白酪氨酸激酶 凋亡 血管生成 c-RET c-Met/HGFR FLT Src TAM Receptor Tyro3 inhibit SGI 7079 Inhibitor Axl Mer SGI7079 inhibitor