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AG 1478 hydrochloride

Catalog #: 1276
20 Citations Datasheet
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AG 1478 hydrochloride | CAS No. 170449-18-0 | EGF Receptor Inhibitors
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Description: Highly potent EGFR-kinase inhibitor
Alternative Names: Tyrphostin AG 1478

Chemical Name: N-(3-Chlorophenyl)-6,7-dimethoxy-4-quinazolinanine hydrochloride

Purity: ≥98%

Product Details
Citations (20)
Supplemental Products
Reviews
Biological Activity Technical Data Additional Information Background Product Datasheets Calculators

Biological Activity

AG 1478 hydrochloride is a 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.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Additional Information

Licensing Caveats:
Sold with the permission of AstraZeneca UK Ltd.

Background References

  1. GPR30 regulates glutamate transporter GLT-1 expression in rat primary astrocytes.
    Lee E, Sidoryk-Wegrzynowicz M, Wang N, Webb A, Son D, Lee K, Aschner M
    J Biol Chem, 2012;287(32):26817-28.
  2. Local Epidermal Growth Factor Receptor Signaling Mediates the Systemic Pathogenic Effects of Staphylococcus aureus Toxic Shock Syndrome

    PLoS ONE, 2016;11(7):e0158969.
  3. EGFR is a pivotal regulator of thrombin-mediated inflammation in primary human nucleus pulposus culture
    BR Huang, TS Chen, DT Bau, IC Chuang, CF Tsai, PC Chang, DY Lu
    Sci Rep, 2017;7(1):8578.
  4. 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).
    Breshears L, Schlievert P, Peterson M
    J Biol Chem, 2012;287(39):32578-87.
  5. A switch role of Src in the biphasic EGF signaling of ER-negative breast cancer cells.
    Zhang, XinTian, Meng, Jun, Wang, Zhao-Yi
    PLoS ONE, 2012;7(8):e41613.
  6. A dangerous liaison: Leptin and sPLA2-IIA join forces to induce proliferation and migration of astrocytoma cells
    R Martín, C Cordova, B Gutiérrez, M Hernández, ML Nieto
    PLoS ONE, 2017;12(3):e0170675.
  7. Characterisation of AmphiAmR11, an amphioxus (Branchiostoma floridae) D2-dopamine-like G protein-coupled receptor.
    Bayliss A, Evans P
    PLoS ONE, 2013;8(11):e80833.
  8. 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
  9. 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
  10. Tyrosine kinase inhibition: an approach to drug development.
    Levitzki and Gazit
    Science, 1995;267:1782
  11. 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

Product Datasheets

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Citations for AG 1478 hydrochloride

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

20 Citations: Showing 1 - 10

  1. Hypoxia-inducible factor 2-alpha-dependent induction of amphiregulin dampens myocardialischemia-reperfusion injury.
    Authors: Koeppen
    Nat Commun  2018;9(1):816
  2. FGF2-dependent mesenchyme and laminin-111 are niche factors in salivary gland organoids.
    Authors: Hosseini Et al.
    J Cell Sci  2018;131
  3. Epidermal Growth Factor Receptor Signaling Enhances the Proinflammatory Effects of Staphylococcus aureus Gamma-Toxin on the Mucosa.
    Authors: Gillman Et al.
    Toxins (Basel)  2017;9
  4. Increased NRG1-ErbB4 signaling in human symptomatic epilepsy
    Authors: Zhu
    Sci Rep  2017;7(1):141
  5. Tissue-type plasminogen activator exerts EGF-like chemokinetic effects on oligodendrocytes in white matter (re)myelination.
    Authors: Leonetti Et al.
    Mol Neurodegener  2017;12:20
  6. 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
  7. Feedback circuitry between miR-218 repression and RTK activation in glioblastoma.
    Authors: Mathew Et al.
    Cell Death Dis  2015;8:ra42
  8. 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
  9. Neuregulin 1 signalling modulates mGluR1 function in mesencephalic dopaminergic neurons.
    Authors: Ledonne Et al.
    Mol Psychiatry  2015;20:959
  10. TrkB interacts with ErbB4 and regulates NRG1-induced NR2B phosphorylation in cortical neurons before synaptogenesis.
    Authors: Pandya and Pillai
    Sci Signal  2014;12:47
  11. Characterisation of AmphiAmR11, an amphioxus (Branchiostoma floridae) D2-DA-like G protein-coupled receptor.
    Authors: Bayliss and Evans
    PLoS One  2013;8:e80833
  12. EMT-induced stemness and tumorigenicity are fueled by the EGFR/Ras pathway.
    Authors: Voon Et al.
    PLoS One  2013;8:e70427
  13. 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
  14. 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
  15. 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
  16. DA-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
  17. Resonant waveguide grating biosensor for living cell sensing.
    Authors: Fang Et al.
    Biophys J  2006;91:1925
  18. 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
  19. The G protein-coupled receptor GPR30 mediates c-fos up-regulation by 17beta-OE and phytoestrogens in breast cancer cells.
    Authors: Maggiolini Et al.
    J Biol Chem  2004;279:27008
  20. IL-13-induced changes in the goblet cell density of human bronchial epithelial cell cultures: MAP kinase and phosphatidylinositol 3-kinase regulation.
    Authors: Atherton Et al.
    Am J Physiol Lung Cell Mol Physiol  2003;285:L730

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