AG 1478 hydrochloride

Cat. No. 1276

AG 1478 hydrochloride C16H14ClN3O2.HCl [170449-18-0]

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Alternative Name: 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).

Licensing Information

Sold with the permission of AstraZeneca UK Ltd.

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.

Certificate of Analysis / Product Datasheet / Safety Datasheet

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.

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.

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 this product please let us know.

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

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.

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.

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

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.

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.

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.

Bayliss and Evans (2013) Characterisation of AmphiAmR11, an amphioxus (Branchiostoma floridae) D2-dopamine-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.

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.

O'Keeffe et al (2009) Dopamine-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.

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.

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

Do you know of a great paper that uses AG 1478 hydrochloride from Tocris? If so please let us know.show all ▼show less ▲

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Keywords: AG 1478 hydrochloride, supplier, potent, EGFR-kinase, inhibitors, inhibits, Epidermal, Growth, Factors, Receptors, ErbB, Her, Receptor, Tyrosine, Kinases, RTKs, AG1478, hydrochloride, Tyrphostin, AstraZeneca, Tocris Bioscience, EGFR Inhibitor products

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