Tyrphostin AG 1296

For research use only.

Catalog No.S8024 Synonyms: AG 1296

6 publications

Tyrphostin AG 1296 Chemical Structure

Molecular Weight(MW): 266.29

Tyrphostin AG 1296 is an inhibitor of PDGFR with IC50 of 0.3-0.5 μM, no activity to EGFR.

Size Price Stock Quantity  
10mM (1mL in DMSO) USD 160 In stock
USD 147 In stock
USD 370 In stock
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Selleck's Tyrphostin AG 1296 has been cited by 6 publications

1 Customer Review

  • After inoculation with KAT4 cells, administration of compounds including MK-2206 (100 mg/kg), tyrphostin AG 1296 (100 mg/kg), or a combination of MK-2206 (100 mg/kg) and tyrphostin AG 1296 (100 mg/kg) was performed. The combination of MK-2206 and tyrphostin AG 1296 induced significant apoptosis of KAT4 tumor cells in vivo measured by the terminal deoxynucleotidyl transferase dUTP nick end labeling assay (green), and nuclei were stained with Hoechst (blue).

    Onco Targets Ther 2014 7, 425-32. Tyrphostin AG 1296 purchased from Selleck.

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Biological Activity

Description Tyrphostin AG 1296 is an inhibitor of PDGFR with IC50 of 0.3-0.5 μM, no activity to EGFR.
PDGFR [1] c-Kit (Swiss 3T3) [1] FGFR (Swiss 3T3) [1]
0.3 μM-0.5 μM 1.8 μM 12.3 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. [1] 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. [2]


Kinase Assay:[1]
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Membrane Autophosphorylation Assays:

Membranes are prepared from confluent cultures of Swiss 3T3 cells as described. For measuring receptor autophosphorylation, 10μg membrane protein per assay are incubated for 20 min on ice in the presence of 1.2μg/mL EGF or 2μg/mL PDGF, or both; 50 mM Hepes (pH 7.5); and 3 mM MnCl2 in a volume of 45μl. In order to test the effects of tyrphostins, these are added in a volume of 0.5 μl (in DMSO; final concentration, 0.5%) 15 min before addition of the growth factors. Phosphorylation is initiated by addition of [γ-32P]ATP and terminated after 2 min by addition of 10μL of a solution containing 6% SDS, 30%β-mercatoethanol, 40% glycerol, and 0.5 mg/mL bromophenol blue. The samples are heated for 5 min at 95 ℃ and subjected to SDS-PAGE using 10% acrylamide gels. The gels are stained and dried and subjected to autoradiographic analysis.
Cell Research:[1]
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  • 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
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 6 mg/mL (22.53 mM)
Water Insoluble
Ethanol Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 266.29


CAS No. 146535-11-7
Storage powder
in solvent
Synonyms AG 1296
Smiles COC1=CC2=NC=C(N=C2C=C1OC)C3=CC=CC=C3

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID