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Submit ReviewAG 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.
M. Wt | 397.47 |
Formula | C19H15N3O3S2 |
Storage | Store at +4°C |
CAS Number | 149092-50-2 |
PubChem ID | 6091659 |
InChI Key | KXDONFLNGBQLTN-WUXMJOGZSA-N |
Smiles | COC1=CC(\C=C(/C#N)C(N)=O)=CC(CSC2=NC3=C(S2)C=CC=C3)=C1O |
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.
Solvent | Max Conc. mg/mL | Max Conc. mM | |
---|---|---|---|
Solubility | |||
DMSO | 39.75 | 100 |
The following data is based on the product molecular weight 397.47. 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.
Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 2.52 mL | 12.58 mL | 25.16 mL |
5 mM | 0.5 mL | 2.52 mL | 5.03 mL |
10 mM | 0.25 mL | 1.26 mL | 2.52 mL |
50 mM | 0.05 mL | 0.25 mL | 0.5 mL |
References are publications that support the biological activity of the product.
Gazit et al (1993) Tyrphostins. 3. Structure-activity relationship studies of α-substituted benzylidenemalononitrile 5-S-aryltyrphostins. J.Med.Chem. 36 3556 PMID: 7902440
Murillo et al (2001) Tyrphostin AG825 triggers p38 mitogen-activated protein kinase-dependent apoptosis in androgen-independent prostate cancer cells C4 and C4-21. Cancer Res. 61 7408 PMID: 11606371
Osherov et al (1993) Selective inhibition of the epidermal growth factor and HER2/Neu receptors by tyrphostins. J.Biol.Chem. 268 11134 PMID: 8098709
If you know of a relevant reference for AG 825, please let us know.
Keywords: AG 825, AG 825 supplier, Selective, ErbB2, inhibitors, inhibits, Epidermal, Growth, Factors, Receptors, ErbB, Her, EGFR, Receptor, Tyrosine, Kinases, RTKs, AG825, Tyrphostin, AG, 825, 1555, Tocris Bioscience
Citations are publications that use Tocris products. Selected citations for AG 825 include:
Lucchetti et al (2013) The prolyl isomerase Pin1 acts synergistically with CDK2 to regulate the basal activity of estrogen receptor α in breast cancer. PLoS One 8 e55355 PMID: 23390529
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
Kedrin et al (2009) ERBB1 and ERBB2 have distinct functions in tumor cell invasion and intravasation. Clin Cancer Res 15 3733 PMID: 19458057
Wu et al (2016) Neuregulin1-β decreases interleukin-1β-induced RhoA activation, myosin light chain phosphorylation, and endothelial hyperpermeability. J Neurochem 136 250 PMID: 26438054
Lee et al (2014) Neuregulin autocrine signaling promotes self-renewal of breast tumor-initiating cells by triggering HER2/HER3 activation. Cancer Res 74 341 PMID: 24177178
Do you know of a great paper that uses AG 825 from Tocris? Please let us know.
Average Rating: 5 (Based on 1 Review.)
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Used in vitro to investigate ERG pathways