Catalog Number: 1276
Alternate Names: Tyrphostin AG 1478
Chemical Name: N-(3-Chlorophenyl)-6,7-dimethoxy-4-quinazolinanine hydrochloride
Biological Activity
Potent and selective inhibitor of epidermal growth factor receptor kinase (IC50 values 3 nM for EGFR and > 100 μM for ErbB2 and PDGFR). Inhibits proliferation of NCI-H2170 NSCLC cells in vitro (IC50 = 1 μM).
Technical Data
  • M.Wt:
    352.22
  • Formula:
    C16H14ClN3O2.HCl
  • Solubility:
    Soluble to 10 mM in DMSO with gentle warming
  • Purity:
    >98%
  • Storage:
    Desiccate at -20°C
  • CAS No:
    170449-18-0
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis. All Tocris products are intended for laboratory research use only.
Additional Information
Licensing Caveats:
Sold with the permission of AstraZeneca UK Ltd.
Background References
  1. Calcium-dependent epidermal growth factor receptor transactivation mediates the angiotensin II-induced mitogen-activated protein kinase activation in vascular smooth muscle cells.
    Eguchi et al.
    J.Biol.Chem., 1998;273:8890
  2. Tyrphostin AG 1478 preferentially inhibits human glioma cells expressing truncated rather than wild-type epidermal growth factor receptors.
    Han et al.
    Cancer Res., 1996;56:3859
  3. Tyrosine kinase inhibition: an approach to drug development.
    Levitzki and Gazit
    Science, 1995;267:1782
  4. Synergism of EGFR and c-Met pathways, cross-talk and inhibition, in non-small cell lung cancer.
    Puri and Salgia
    J.Carcinog., 2008;7:9
Citations:

The citations listed below are publications that use Tocris products. Selected citations for AG 1478 hydrochloride include:

13 Citations: Showing 1 - 10
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  1. Increased NRG1-ErbB4 signaling in human symptomatic epilepsy
    Authors: Zhu
    Sci Rep 2017;7(1):141
  2. Local Epidermal Growth Factor Receptor Signaling Mediates the Systemic Pathogenic Effects of Staphylococcus aureus Toxic Shock Syndrome
    Authors: Breshears Et al.
    PLoS One 2016;11:e0158969
  3. Feedback circuitry between miR-218 repression and RTK activation in glioblastoma.
    Authors: Mathew Et al.
    Cell Death Dis 2015;8:ra42
  4. Conformations of tissue plasminogen activator (tPA) orchestrate neuronal survival by a crosstalk between EGFR and NMDAR.
    Authors: Bertrand Et al.
    Sci Rep 2015;6:e1924
  5. TrkB interacts with ErbB4 and regulates NRG1-induced NR2B phosphorylation in cortical neurons before synaptogenesis.
    Authors: Pandya and Pillai
    Sci Signal 2014;12:47
  6. Characterisation of AmphiAmR11, an amphioxus (Branchiostoma floridae) D2-dopamine-like G protein-coupled receptor.
    Authors: Bayliss and Evans
    PLoS One 2013;8:e80833
  7. EMT-induced stemness and tumorigenicity are fueled by the EGFR/Ras pathway.
    Authors: Voon Et al.
    PLoS One 2013;8:e70427
  8. Activation of ErbB2 and Downstream Signalling via Rho Kinases and ERK1/2 Contributes to Diabetes-Induced Vascular Dysfunction.
    Authors: Akhtar Et al.
    PLoS One 2013;8:e67813
  9. Profiling epidermal growth factor receptor and heregulin receptor 3 heteromerization using receptor tyrosine kinase heteromer investigation technology.
    Authors: Ayoub Et al.
    PLoS One 2013;8:e64672
  10. A disintegrin and metalloproteinase 17 (ADAM17) and epidermal growth factor receptor (EGFR) signaling drive the epithelial response to Staphylococcus aureus toxic shock syndrome toxin-1 (TSST-1).
    Authors: Breshears Et al.
    J Biol Chem 2012;287:32578
  11. Dopamine-induced proliferation of adult neural precursor cells in the mammalian subventricular zone is mediated through EGF.
    Authors: O'Keeffe Et al.
    Proc Natl Acad Sci U S A 2009;106:8754
  12. Rapid estrogenic regulation of extracellular signal- regulated kinase 1/2 signaling in cerebellar granule cells involves a G protein- and protein kinase A-dependent mechanism and intracellular activation of protein phosphatase 2A.
    Authors: Belcher Et al.
    Endocrinology 2005;146:5397
  13. The G protein-coupled receptor GPR30 mediates c-fos up-regulation by 17beta-estradiol and phytoestrogens in breast cancer cells.
    Authors: Maggiolini Et al.
    J Biol Chem 2004;279:27008
Expand to show all 13 Citations

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