1. Protein Tyrosine Kinase/RTK
    Apoptosis
  2. PDGFR
    c-Kit
    FLT3
    Apoptosis
  3. Tyrphostin AG1296

Tyrphostin AG1296 (Synonyms: AG1296)

Cat. No.: HY-13894
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Tyrphostin AG1296 is a potent and selective inhibitor of platelet-derived growth factor receptor (PDGFR), with an IC50 of 0.8 μM. Tyrphostin AG1296 inhibits signaling of human PDGF α- and β-receptors as well as of the related stem cell factor receptor (c-Kit). Tyrphostin AG1296 is also a potent inhibitor of FLT3, with an IC50 in the micromolar range.

For research use only. We do not sell to patients.

Tyrphostin AG1296 Chemical Structure

Tyrphostin AG1296 Chemical Structure

CAS No. : 146535-11-7

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Description

Tyrphostin AG1296 is a potent and selective inhibitor of platelet-derived growth factor receptor (PDGFR), with an IC50 of 0.8 μM. Tyrphostin AG1296 inhibits signaling of human PDGF α- and β-receptors as well as of the related stem cell factor receptor (c-Kit). Tyrphostin AG1296 is also a potent inhibitor of FLT3, with an IC50 in the micromolar range[1][2][3].

IC50 & Target[2]

PDGFRα

 

PDGFRβ

 

In Vitro

Tyrphostin AG1296 (0.625-20 μM; 72 h) suppresses viability of PLX4032-resistant melanoma cells[4].
Tyrphostin AG1296 (2.5-20 μM; 48 h) induces apoptosis of A375R cells[4].
Tyrphostin AG1296 (5 and 20 μM; 2 h) inhibits PDGFR phosphorylation in A375R cells[4].
Tyrphostin AG1296 (0.0625-1 μM; 8 h) inhibits migration of A375R cells[4].

Cell Viability Assay[4]

Cell Line: PLX4032-resistant cell lines (A375R and SK-MEL-5R)
Concentration: 0.625, 1.25, 5, 20 μM
Incubation Time: 72 h
Result: Reduced the viability of both PLX4032-sensitive and PLX4032-resistant cell lines.

Apoptosis Analysis[4]

Cell Line: A375R cells
Concentration: 2.5, 5, 10, 20 μM
Incubation Time: 48 h
Result: Induced dramatic apoptosis in A375R cells.

Western Blot Analysis[4]

Cell Line: A375R cells
Concentration: 5, 20 μM
Incubation Time: 2 h
Result: Inhibited phosphorylation of both PDGFR-α and PDGFR-β.
In Vivo

Tyrphostin AG1296 (40 and 80 mg/kg; i.p. daily for two weeks) suppresses A375R tumor growth in vivo[4].
Tyrphostin AG1296 (2 mg/kg; i.p. every other day for 3 weeks) inhibits the atherosclerotic plaque progression and enhances plaque stability by inhibiting inflammatory responses, reducing the expression of matrix metalloproteinases and promoting macrophages from proinflammatory phenotype to anti-inflammatory phenotype[5].

Animal Model: Nud/nud mice are injected with A375R cells[4]
Dosage: 40, 80 mg/kg
Administration: I.p. daily for two weeks
Result: Led to an intermediate level of tumor growth suppression at dose of 40 mg/kg, and significant inhibition of A375R tumor growth at dose of 80 mg/kg.
Well tolerated by healthy mice without significant signs of overt toxicity or weight loss.
Molecular Weight

266.29

Formula

C₁₆H₁₄N₂O₂

CAS No.

146535-11-7

SMILES

COC1=C(OC)C=C2N=CC(C3=CC=CC=C3)=NC2=C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
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Keywords:

Tyrphostin AG1296AG1296Tyrphostin AG 1296Tyrphostin AG-1296AG 1296AG-1296PDGFRc-KitFLT3ApoptosisPlatelet-derived growth factor receptorSCFRCD117Cluster of differentiation antigen 135CD135Fms like tyrosine kinase 3platelet-derivedgrowthfactorPDGFαβstemcellInhibitorinhibitorinhibit

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Tyrphostin AG1296
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