PD 158780

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Cat.No. 2615 - PD 158780 | C14H12BrN5 | CAS No. 171179-06-9
Description: Potent ErbB receptor family inhibitor
Chemical Name: N4-(3-Bromophenyl)-N6-methyl-pyrido[3,4-d]pyrimidine-4,6-diamine
Purity: ≥99% (HPLC)
Datasheet
Citations (2)
Reviews (1)
Literature (4)

Biological Activity for PD 158780

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.

Compound Libraries for PD 158780

PD 158780 is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.

Technical Data for PD 158780

M. Wt 330.18
Formula C14H12BrN5
Storage Store at -20°C
Purity ≥99% (HPLC)
CAS Number 171179-06-9
PubChem ID 4707
InChI Key KFHMLBXBRCITHF-UHFFFAOYSA-N
Smiles CNC1=NC=C2N=CN=C(NC3=CC=CC(Br)=C3)C2=C1

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.

Solubility Data for PD 158780

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 33.01 100
ethanol 8.25 25

Preparing Stock Solutions for PD 158780

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.

Select a batch to recalculate based on the batch molecular weight:
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

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References for PD 158780

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.

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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

2 Citations for PD 158780

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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Reviews for PD 158780

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Bath application in whole cell recording.
By Anonymous on 12/11/2017
Assay Type: In Vitro
Species: Mouse

Electrophysiology whole cell recordings and it worked as expected.

Coating our tubing with BSA helped to prevent the staining that occurred with this compound.


Literature in this Area

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