PD 158780
Chemical Name: N4-(3-Bromophenyl)-N6-methyl-pyrido[3,4-d]pyrimidine-4,6-diamine
Purity: ≥99%
Biological Activity
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.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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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.
Fry et al.
Biochem.Pharmacol., 1997;54:877 -
Growth inhibition of nasopharyngeal carcinoma cells by EGF receptor tyrosine kinase inhibitors.
Sun et al.
Anticancer Res., 1999;19:919 -
G1 cell cycle arrest due to inhibition of erbB family receptor tyrosine kinases does not require the retinoblastoma protein.
Gonzales et al.
Exp.Cell Res., 2005;303:56
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Citations for PD 158780
The citations listed below are publications that use Tocris products. Selected citations for PD 158780 include:
2 Citations: Showing 1 - 2
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Radial glia regulate vascular patterning around the developing spinal cord.
Authors: Matsuoka Et al.
Elife 2016;5
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Neuregulin 1 signalling modulates mGluR1 function in mesencephalic dopaminergic neurons.
Authors: Ledonne Et al.
Mol Psychiatry 2015;20:959
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Electrophysiology whole cell recordings and it worked as expected.
Coating our tubing with BSA helped to prevent the staining that occurred with this compound.