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Tyrphostin AG1296

Catalog No. T6711 CAS 146535-11-7

Synonyms: Tyrphostin AG 1296, AG 1296

Tyrphostin AG1296 (Tyrphostin AG 1296) is an inhibitor of PDGFR with IC50 of 0.3-0.5 μM, no activity to EGFR.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.

Tyrphostin AG1296, CAS 146535-11-7

Pack Size	Availability	Price/USD
1 mg	In stock	$ 40.00
5 mg	In stock	$ 89.00
10 mg	In stock	$ 153.00
25 mg	In stock	$ 317.00
50 mg	In stock	$ 490.00
100 mg	In stock	$ 723.00
500 mg	In stock	$ 1,520.00
1 mL * 10 mM (in DMSO)	In stock	$ 123.00

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Purity: 99.68%

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Description	Tyrphostin AG1296 (Tyrphostin AG 1296) is an inhibitor of PDGFR with IC50 of 0.3-0.5 μM, no activity to EGFR.
Targets&IC50	c-Kit (Swiss 3T3):1.8 μM, FGFR (Swiss 3T3):12.3 μM, PDGFR:0.3 μM-0.5 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.
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

Synonyms	Tyrphostin AG 1296, AG 1296
Molecular Weight	266.29
Formula	C16H14N2O2
CAS No.	146535-11-7

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 6 mg/mL (22.53 mM)

H2O: < 1 mg/mL (insoluble or slightly soluble)

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

References and Literature

1. Kovalenko M, et al. Cancer Res, 1994, 54(23), 6106-6114. 2. Kovalenko M, et al. Biochemistry, 1997, 36(21), 6260-6269.

Related compound libraries

This product is contained In the following compound libraries：

Tyrosine Kinase Inhibitor Library Inhibitor Library Kinase Inhibitor Library Anti-Cancer Active Compound Library Reprogramming Compound Library Anti-Pancreatic Cancer Compound Library Angiogenesis related Compound Library Human Metabolite Library Apoptosis Compound Library Anti-Cancer Compound Library

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Keywords

Tyrphostin AG1296 146535-11-7 Angiogenesis Apoptosis Tyrosine Kinase/Adaptors c-Kit PDGFR FLT FGFR Fms like tyrosine kinase 3 PDGF AG-1296 CD117 inhibit platelet-derived CD135 SCFR Tyrphostin AG-1296 FLT3 cell growth stem Inhibitor Cluster of differentiation antigen 135 Tyrphostin AG 1296 AG 1296 factor Platelet-derived growth factor receptor AG1296 inhibitor

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