An inhibitor of PDGF receptor kinase
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AG-1296

Item No. 10010592

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
6,7-dimethoxy-2-phenyl-quinoxaline
CAS Number
146535-11-7
Synonyms
  • Tyrphostin AG-1296
Molecular Formula
C16H14N2O2
Formula Weight
266.3
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 5 mg/mlDMF:PBS (pH 7.2) (1:2): 0.3 mg/mlDMSO: 3 mg/ml
λmax
233, 264, 367 nm
SMILES
COc1cc2nc(cnc2cc1OC)c1ccccc1
InChi Code
InChI=1S/C16H14N2O2/c1-19-15-8-12-13(9-16(15)20-2)18-14(10-17-12)11-6-4-3-5-7-11/h3-10H,1-2H3
InChi Key
QNOXYUNHIGOWNY-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $31

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    5 mg

    $129

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    10 mg

    $228

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    25 mg

    $493

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    Product Description

    Protein tyrosine kinase (PTK) inhibitors are potential antiproliferative agents for diseases caused by the hyperactivity of PTKs. Tyrphostins are a class of antiproliferative compounds which act as PTK blockers. PTK inhibitors specific for platelet-derived growth factor (PDGF) receptor kinase could help in the treatment of atherosclerosis, restenosis, pulmonary fibrosis, and gliomas.1 AG-1296 is a potent and selective inhibitor of PDGF receptor kinase with an IC50 value of about 0.4 µM both in vitro and in cells (Swiss 3T3 cells).2 It inhibits ligand-stimulated DNA synthesis in platelet-derived growth factor receptor and stem cell factor/kit receptor transfected cells with an IC50 values of 1.5 and 1.8 µM, respectively. 2 Treatment of sis oncogene transfected NIH3T3 cells with AG-1296 reverses the transformed phenotype.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Levitzki, A., and Gazit, A. Tyrosine kinase inhibition: An approach to drug development. Science 267(5205), 1782-1788 (1995).

    2. Kovalenko, M., Gazit, A., Böhmer, A., et al. Selective platelet-derived growth factor receptor kinase blockers reverse sis-transformation. Cancer Res. 54(23), 6106-6114 (1994).

    Product Citations

    Han, J.-H., Heo, K.-S., and Myung, C.-S. Cytokine-induced apoptosis inhibitor 1 (CIAPIN1) accelerates vascular remodelling via p53 and JAK2-STAT3 regulation in vascular smooth muscle cells. Br. J. Pharmacol. 178(22), 4533-4551 (2021).

    Roach, E.E., Chakrabarti, R., Park, N.I., et al. Intrinsic regulation of hemangioma involution by platelet-derived growth factor. Cell Death Dis. 3, e328 (2012).