Tyrphostin AG 1296

Catalog No.S8024

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

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Tyrphostin AG 1296 Chemical Structure

Tyrphostin AG 1296 Chemical Structure
Molecular Weight: 266.29

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Product Information

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Product Description

Biological Activity

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

Protocol(Only for Reference)

Kinase Assay: [1]

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 Assay: [1]

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

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDog
Weight (kg)0.020.151.80.40.0810
Body Surface Area (m2)0.0070.0250.150.050.020.5
Km factor36128520
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

References

[1] Kovalenko M, et al. Cancer Res, 1994, 54(23), 6106-6114.

[2] Kovalenko M, et al. Biochemistry, 1997, 36(21), 6260-6269.

Chemical Information

Download Tyrphostin AG 1296 SDF
Molecular Weight (MW) 266.29
Formula

C16H14N2O2

CAS No. 146535-11-7
Storage 3 years -20℃powder
6 months-80℃in solvent
Synonyms AG 1296
Solubility (25°C) * In vitro DMSO 6 mg/mL (22.53 mM)
Water <1 mg/mL (<1 mM)
Ethanol <1 mg/mL (<1 mM)
* <1 mg/ml means slightly soluble or 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 Name Quinoxaline, 6,7-dimethoxy-2-phenyl-

Customer Product Validation(1)


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Rating
Source Onco Targets Ther 2014 7, 425-32. Tyrphostin AG 1296 purchased from Selleck
Method Terminal deoxynucleotidyl transferase dUTP nick end labeling assay/Hoechst
Cell Lines KAT4 tumor cells
Concentrations 100 mg/kg
Incubation Time 2 weeks
Results Though tyrphostin AG 1296 enhanced apoptotic in tumors, the combination with MK-2206 induced more significant apoptotic characteristics in tumors than either MK-2206 or tyrphostin AG 1296 alone as measured using TUNEL and nuclei staining assays.

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Tel: +1-832-582-8158 Ext:3

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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