Home Protein Tyrosine Kinase PDGFR inhibitor - c-Kit inhibitor - FGFR inhibitor - Apoptosis related activator Tyrphostin AG 1296 For research use only.

Tyrphostin AG 1296

Synonyms: AG 1296

Tyrphostin AG 1296 is an inhibitor of PDGFR with IC50 of 0.3-0.5 μM, no activity to EGFR. Tyrphostin AG1296 inhibits FGFR and c-Kit with IC50 of 12.3 μM and 1.8 μM in Swiss 3T3 cells. Tyrphostin AG1296 induces dramatic apoptosis in A375R cells.

Tyrphostin AG 1296 Chemical Structure

Tyrphostin AG 1296 Chemical Structure

CAS No. 146535-11-7

Purity & Quality Control

Batch: S802401 DMSO]6 mg/mL]false]Water]Insoluble]false]Ethanol]Insoluble]false Purity: 99.90%
99.90

Tyrphostin AG 1296 Related Products

Signaling Pathway

PDGFR Signaling Pathways

PDGFR Signaling Pathway

Biological Activity

Description Tyrphostin AG 1296 is an inhibitor of PDGFR with IC50 of 0.3-0.5 μM, no activity to EGFR. Tyrphostin AG1296 inhibits FGFR and c-Kit with IC50 of 12.3 μM and 1.8 μM in Swiss 3T3 cells. Tyrphostin AG1296 induces dramatic apoptosis in A375R cells.
Targets
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
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 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 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

Chemical Information & Solubility

Molecular Weight 266.29 Formula

C16H14N2O2
CAS No. 146535-11-7 SDF Download Tyrphostin AG 1296 SDF
Smiles COC1=C(C=C2C(=C1)N=CC(=N2)C3=CC=CC=C3)OC
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 6 mg/mL ( (22.53 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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