Tyrphostin AG 1296
Product Description
Molecular Weight: 266.29 Tyrphostin AG 1296 is an inhibitor of PDGFR with IC50 of 0.3-0.5 μM, no activity to EGFR.
Biological Activity
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.
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.
Contact us if you need more details on 146535-11-7. We are ready to answer your questions on packaging, logistics, certification or any other aspects about Tyrphostin AG 1296 146535-11-7、Tyrphostin AG 1296. If these products fail to match your need, please contact us and we would like to provide relevant information.
Biological Activity
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.
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.
Contact us if you need more details on 146535-11-7. We are ready to answer your questions on packaging, logistics, certification or any other aspects about Tyrphostin AG 1296 146535-11-7、Tyrphostin AG 1296. If these products fail to match your need, please contact us and we would like to provide relevant information.
Product Categories : Protein Tyrosine Kinase > PDGFR Inhibitor
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