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
Literature

Biological Activity

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.

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Technical Data

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.

All Tocris products are intended for laboratory research use only.

Solubility Data

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

Preparing Stock Solutions

The following data is based on the product molecular weight 330.18. Batch specific molecular weights may vary from batch to batch due to solvent 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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Product Datasheets

Safety Datasheet

References

References are publications that support the products' biological activity.

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


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