Home Protein Tyrosine Kinase PDGFR inhibitor - c-Kit inhibitor - FGFR inhibitor - Apoptosis related activator Tyrphostin AG 1296

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Tyrphostin AG 1296 PDGFR inhibitor

Cat.No.S8024

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 PDGFR inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 266.29

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Quality Control

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

Chemical Information, Storage & Stability

Molecular Weight 266.29 Formula

C16H14N2O2

 Storage (From the date of receipt)
CAS No. 146535-11-7 Download SDF Storage of Stock Solutions

Synonyms AG 1296 Smiles COC1=C(C=C2C(=C1)N=CC(=N2)C3=CC=CC=C3)OC

Solubility

In vitro
Batch:

DMSO : 6 mg/mL (22.53 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

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In vivo
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Mechanism of Action

Targets/IC50/Ki
PDGFR [1]
0.3 μM-0.5 μM
c-Kit (Swiss 3T3) [1]
1.8 μM
FGFR (Swiss 3T3) [1]
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
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.
References

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