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PD 158780 is a potent inhibitor of ErbB receptor family tyrosine kinases (IC50 values are 0.008, 49 and 52 nM for EGFR, ErbB2 and ErbB2/ErbB4 respectively) that does not inhibit FGF or PDGF-mediated tyrosine phosphorylation. Induces G1 cell cycle arrest in MCF10A cells and is antiproliferative in A431 human epidermal carcinoma cells.
PD 158780 is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.
|Storage||Store at -20°C|
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|
The following data is based on the product molecular weight 330.18. 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||3.03 mL||15.14 mL||30.29 mL|
|5 mM||0.61 mL||3.03 mL||6.06 mL|
|10 mM||0.3 mL||1.51 mL||3.03 mL|
|50 mM||0.06 mL||0.3 mL||0.61 mL|
References are publications that support the biological activity of the product.
Fry et al (1997) Biochemical and antiproliferative properties of 4-[ar(alk)ylmino]pyridopyrimidines, a new chemical class of potent and specific epidermal growth factor receptor tyrosine kinase inhibitor. Biochem.Pharmacol. 54 877 PMID: 9354588
Sun et al (1999) Growth inhibition of nasopharyngeal carcinoma cells by EGF receptor tyrosine kinase inhibitors. Anticancer Res. 19 919 PMID: 10368634
Gonzales et al (2005) G1 cell cycle arrest due to inhibition of erbB family receptor tyrosine kinases does not require the retinoblastoma protein. Exp.Cell Res. 303 56 PMID: 15572027
If you know of a relevant reference for PD 158780, please let us know.
Keywords: PD 158780, PD 158780 supplier, Potent, ErbB, receptor, family, inhibitors, inhibits, Epidermal, Growth, Factors, Receptors, Her, EGFR, Receptor, Tyrosine, Kinases, RTKs, PD158780, 2615, Tocris Bioscience
Citations are publications that use Tocris products. Selected citations for PD 158780 include:
Matsuoka et al (2016) Radial glia regulate vascular patterning around the developing spinal cord. Elife 5 PMID: 27852438
Ledonne et al (2015) Neuregulin 1 signalling modulates mGluR1 function in mesencephalic dopaminergic neurons. Mol Psychiatry 20 959 PMID: 25266126
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Schizophrenia is a debilitating psychiatric disorder that affects 1% of the worldwide population. This poster describes the neurobiology of Schizophrenia, as well as highlighting the genetic and environmental factors that play a fundamental role in the etiology of the disease. The current and emerging drug targets are also discussed.