AG 825
Chemical Name: 3-[3-[(2-Benzothiazolylthio)methyl]-4-hydroxy-5-methoxyphenyl]-2-cyano-2-propenamide
Biological Activity
AG 825 is a selective ErbB2 inhibitor (IC50 values are 0.15 and 19 μM at ErbB2 and ErbB1 respectively). Preferentially triggers p38 MAP kinase-dependent apoptosis in androgen-independent prostate cancer cells.Technical Data
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.
Background References
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Tyrphostins. 3. Structure-activity relationship studies of α-substituted benzylidenemalononitrile 5-S-aryltyrphostins.
Gazit et al.
J.Med.Chem., 1993;36:3556 -
Selective inhibition of the epidermal growth factor and HER2/Neu receptors by tyrphostins.
Osherov et al.
J.Biol.Chem., 1993;268:11134 -
Tyrphostin AG825 triggers p38 mitogen-activated protein kinase-dependent apoptosis in androgen-independent prostate cancer cells C4 and C4-21.
Murillo et al.
Cancer Res., 2001;61:7408
Product Datasheets
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Citations for AG 825
The citations listed below are publications that use Tocris products. Selected citations for AG 825 include:
5 Citations: Showing 1 - 5
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Neuregulin1-β decreases interleukin-1β-induced RhoA activation, myosin light chain phosphorylation, and endothelial hyperpermeability.
Authors: Wu Et al.
J Neurochem 2016;136:250
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Neuregulin autocrine signaling promotes self-renewal of breast tumor-initiating cells by triggering HER2/HER3 activation.
Authors: Lee Et al.
Cancer Res 2014;74:341
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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
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The prolyl isomerase Pin1 acts synergistically with CDK2 to regulate the basal activity of estrogen receptor α in breast cancer.
Authors: Lucchetti Et al.
PLoS One 2013;8:e55355
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ERBB1 and ERBB2 have distinct functions in tumor cell invasion and intravasation.
Authors: Kedrin Et al.
Clin Cancer Res 2009;15:3733
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