Tyrphostin AG1296

SKU: orb1300533

Description

Tyrphostin AG1296

Research Area

Cardiovascular Research, Cell Biology, Signal Transduction

Key Properties

• CAS Number: 146535-11-7
• MW: 266.29
• Purity: 100.00%
• Formula: C₁₆H₁₄N₂O₂
• SMILES: COc1cc2ncc(nc2cc1OC)-c1ccccc1
• Target: FGFR,c-Kit,PDGFR,Apoptosis,FLT
• Solubility: H2O:< 1 mg/mL (insoluble or slightly soluble);Ethanol:< 1 mg/mL (insoluble or slightly soluble);DMSO:11 mg/mL (41.31 mM);10% DMSO+90% Corn Oil:1 mg/mL (3.76 mM)

Bioactivity

• Target IC50:
  PDGFR:0.3 μM-0.5 μM|FGFR (Swiss 3T3):12.3 μM|c-Kit (Swiss 3T3):1.8 μM
• In Vitro:
  AG 1296 inhibits selectively the PDGF receptor kinase and the PDGF dependent DNA synthesis in Swiss 3T3 cells and in porcine aorta endothellal cells with 50% inhibitory concentrations below 5 and 1μM, respectively. AG1296 inhibits FGFR and c-Kit with IC50 of 12.3 μM and 1.8 μM in Swiss 3T3 cells. AG1296 potently inhibits signaling of human PDGF -α and -β receptors but has no effect on autophosphorylation of the VEGFR KDR or on DNA synthesis induced by VEGF in porcine aortlc endothelial cells. Treatment by AG1296 reverses the transformed phenotype of sis-transfected NIH 3T3 cells but has no effect on src-transformed NIH3T3 cells.AG1296 is an ATP-competitive inhibitor. AG1296 interferes neither with PDGF binding nor with PDGF receptor dimerization while it abolishes PDGF receptor autophosphorylation. Thus, AG1296 is a pure inhibitor of the catalytic activity of the receptor tyrosine kinase.
• Cell Research:
  Cell lines: Swiss 3T3. Concentrations: ~50 μM. Incubation Time: 3 days. Method: Cells are seeded in 24-well plates (5000 cells/well) in DMEM/10% FCS.On the next day the medium is changed to DMEM/2% FcS with or without growth factors and tyrphostins are added as indicated.Three days later the cells are counted in a hemocytometer

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

SCFR, stem, Tyrphostin AG 1296, Tyrphostin AG1296, Tyrphostin AG-1296, platelet-derived, Platelet-derived growth factor receptor, PDGF, PDGFR, inhibit, Inhibitor, FLT3, growth, factor, Fms like tyrosine kinase 3, FGFR (Swiss 3T3), AG 1296, AG1296, AG-1296, Apoptosis, CD117, CD135, Cluster of differentiation antigen 135, cKit, c-Kit, c-Kit (Swiss 3T3), cell

Compound Identifiers

PubChem CID

2049