SGI-7079

SKU: orb1300290

Description

SGI-7079

Research Area

Cardiovascular Research, Cell Biology, Signal Transduction

Key Properties

• CAS Number: 1239875-86-5
• MW: 455.53
• Purity: 98.70%
• Formula: C₂₆H₂₆FN₇
• SMILES: CN1CCN(CC1)c1ccc(Nc2nc(-c3cccc(CC#N)c3)c3c(C)c[nH]c3n2)cc1F
• Target: FLT,Src,c-Met/HGFR,c-RET,TAM Receptor
• Solubility: DMSO:250 mg/mL (548.81 mM);H2O:< 1 mg/mL (insoluble or slightly soluble);Ethanol:< 1 mg/mL (insoluble or slightly soluble);10% DMSO+40% PEG300+5% Tween 80+45% Saline:3.3 mg/mL (7.24 mM)

Bioactivity

• 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.
• 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.
• 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.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

FLT3, Inhibitor, HGFR, Mer, inhibit, Met, cRET, c-Met, cMet/HGFR, cMet, AXL, Axl, Tyro3, SGI 7079, SGI7079, SGI-7079, Yes, TAM Receptor, TAMReceptor, RET

Compound Identifiers

PubChem CID

46870258