AG 1478 hydrochloride

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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% (HPLC)
Citations (20)
Reviews (2)
Literature (1)

Biological Activity for AG 1478 hydrochloride

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).

Licensing Information

Sold with the permission of AstraZeneca UK Ltd.

Technical Data for AG 1478 hydrochloride

M. Wt 352.22
Formula C16H14ClN3O2.HCl
Storage Desiccate at -20°C
Purity ≥98% (HPLC)
CAS Number 170449-18-0
PubChem ID 3035187
Smiles ClC1=CC(NC2=NC=NC3=C2C=C(OC)C(OC)=C3)=CC=C1.Cl

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.

Solubility Data for AG 1478 hydrochloride

Solvent Max Conc. mg/mL Max Conc. mM
DMSO 3.52 10 with gentle warming

Preparing Stock Solutions for AG 1478 hydrochloride

The following data is based on the product molecular weight 352.22. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
0.1 mM 28.39 mL 141.96 mL 283.91 mL
0.5 mM 5.68 mL 28.39 mL 56.78 mL
1 mM 2.84 mL 14.2 mL 28.39 mL
5 mM 0.57 mL 2.84 mL 5.68 mL

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Product Datasheets for AG 1478 hydrochloride

Certificate of Analysis / Product Datasheet
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References for AG 1478 hydrochloride

References are publications that support the biological activity of the product.

Eguchi et al (1998) Calcium-dependent epidermal growth factor receptor transactivation mediates the angiotensin II-induced mitogen-activated protein kinase activation in vascular smooth muscle cells. J.Biol.Chem. 273 8890 PMID: 9535870

Han et al (1996) Tyrphostin AG 1478 preferentially inhibits human glioma cells expressing truncated rather than wild-type epidermal growth factor receptors. Cancer Res. 56 3859 PMID: 8752145

Puri and Salgia (2008) Synergism of EGFR and c-Met pathways, cross-talk and inhibition, in non-small cell lung cancer. J.Carcinog. 7 9 PMID: 19240370

Levitzki and Gazit (1995) Tyrosine kinase inhibition: an approach to drug development. Science 267 1782 PMID: 7892601

If you know of a relevant reference for AG 1478 hydrochloride, please let us know.

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20 Citations for AG 1478 hydrochloride

Citations are publications that use Tocris products. Selected citations for AG 1478 hydrochloride include:

Leonetti et al (2017) Tissue-type plasminogen activator exerts EGF-like chemokinetic effects on oligodendrocytes in white matter (re)myelination. Mol Neurodegener 12 20 PMID: 28231842

Mathew et al (2015) Feedback circuitry between miR-218 repression and RTK activation in glioblastoma. Cell Death Dis 8 ra42 PMID: 25943352

Bertrand et al (2015) Conformations of tissue plasminogen activator (tPA) orchestrate neuronal survival by a crosstalk between EGFR and NMDAR. Sci Rep 6 e1924 PMID: 26469972

Pandya and Pillai (2014) TrkB interacts with ErbB4 and regulates NRG1-induced NR2B phosphorylation in cortical neurons before synaptogenesis. Sci Signal 12 47 PMID: 25052836

O'Keeffe et al (2009) DA-induced proliferation of adult neural precursor cells in the mammalian subventricular zone is mediated through EGF. Proc Natl Acad Sci U S A 106 8754 PMID: 19433789

Breshears et al (2016) Local Epidermal Growth Factor Receptor Signaling Mediates the Systemic Pathogenic Effects of Staphylococcus aureus Toxic Shock Syndrome PLoS One 11 e0158969 PMID: 27414801

Maggiolini et al (2004) The G protein-coupled receptor GPR30 mediates c-fos up-regulation by 17beta-OE and phytoestrogens in breast cancer cells. J Biol Chem 279 27008 PMID: 15090535

Atherton et al (2003) IL-13-induced changes in the goblet cell density of human bronchial epithelial cell cultures: MAP kinase and phosphatidylinositol 3-kinase regulation. Am J Physiol Lung Cell Mol Physiol 285 L730 PMID: 12794003

Ledonne et al (2015) Neuregulin 1 signalling modulates mGluR1 function in mesencephalic dopaminergic neurons. Mol Psychiatry 20 959 PMID: 25266126

Breshears et al (2012) 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). J Biol Chem 287 32578 PMID: 22833676

Belcher et al (2005) 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. Endocrinology 146 5397 PMID: 16123167

Ayoub et al (2013) Profiling epidermal growth factor receptor and heregulin receptor 3 heteromerization using receptor tyrosine kinase heteromer investigation technology. PLoS One 8 e64672 PMID: 23700486

Akhtar et al (2013) Activation of ErbB2 and Downstream Signalling via Rho Kinases and ERK1/2 Contributes to Diabetes-Induced Vascular Dysfunction. PLoS One 8 e67813 PMID: 23826343

Bayliss and Evans (2013) Characterisation of AmphiAmR11, an amphioxus (Branchiostoma floridae) D2-DA-like G protein-coupled receptor. PLoS One 8 e80833 PMID: 24265838

Voon et al (2013) EMT-induced stemness and tumorigenicity are fueled by the EGFR/Ras pathway. PLoS One 8 e70427 PMID: 23950932

Fang et al (2006) Resonant waveguide grating biosensor for living cell sensing. Biophys J 91 1925 PMID: 16766609

Zhu (2017) Increased NRG1-ErbB4 signaling in human symptomatic epilepsy Sci Rep 7 141 PMID: 28273943

Hosseini et al (2018) FGF2-dependent mesenchyme and laminin-111 are niche factors in salivary gland organoids. J Cell Sci 131 PMID: 29361536

Koeppen (2018) Hypoxia-inducible factor 2-alpha-dependent induction of amphiregulin dampens myocardialischemia-reperfusion injury. Nat Commun 9 816 PMID: 29483579

Gillman et al (2017) Epidermal Growth Factor Receptor Signaling Enhances the Proinflammatory Effects of Staphylococcus aureus Gamma-Toxin on the Mucosa. Toxins (Basel) 9 PMID: 28657583

Do you know of a great paper that uses AG 1478 hydrochloride from Tocris? Please let us know.

Reviews for AG 1478 hydrochloride

Average Rating: 4.5 (Based on 2 Reviews.)

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It works great!.
By Anonymous on 09/17/2022
Assay Type: In Vitro
Species: Mouse
Cell Line/Tissue: Cancer cells

PGE2 secretion was measured in mouse breast cancer cell lines and AG1478 significantly abolished the EGF-induced PGE2 secretion.

review image

EGFR and MAPK inhibitor.
By Anonymous on 03/10/2020
Assay Type: In Vitro
Species: Human
Cell Line/Tissue: Hepg2, Huh7

Used this inhibitor in 50nm for 24 hours and I found less activation of the MAPK pathway and cell growth and migration

serum-free media is working good for me

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Literature in this Area

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Angiogenesis in Cancer Poster

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