PD 158780

Name: PD 158780
Brand: Tocris Bioscience
SKU: 2615
Rating: 4 (1 reviews)

Tocris Bioscience, part of Bio-Techne | Catalog # 2615

Citations (10)

COA / SDS

Potent ErbB receptor family inhibitor

Key Product Details

Description:	Potent ErbB receptor family inhibitor
Chemical Name:	N⁴-(3-Bromophenyl)-N⁶-methyl-pyrido[3,4-d]pyrimidine-4,6-diamine
Purity:	≥99% (HPLC)
Molecular Weight:	330.18

View Full Technical Details for PD 158780

Technical Data
Citations

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 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.

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	0.30 mL	1.51 mL	3.03 mL
50 mM	0.06 mL	0.30 mL	0.61 mL

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References for PD 158780

References are publications that support the biological activity of the product.

Sun Growth inhibition of nasopharyngeal carcinoma cells by EGF receptor tyrosine kinase inhibitors. Anticancer Res. 1999 PMID: 10368634
Gonzales G1 cell cycle arrest due to inhibition of erbB family receptor tyrosine kinases does not require the retinoblastoma protein. Exp.Cell Res. 2005 PMID: 15572027
Fry 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. 1997 PMID: 9354588