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PD 158780

Cat. No. 2615

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Chemical Name: N⁴-(3-Bromophenyl)-N⁶-methyl-pyrido[3,4-d]pyrimidine-4,6-diamine

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.

Technical Data

M.Wt:

330.18

Formula:

C₁₄H₁₂BrN₅

Solubility:

Soluble to 100 mM in DMSO and to 25 mM in ethanol

Purity:

>99 %

Storage:

Store at -20°C

CAS No:

171179-06-9

The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.

Resources

Certificate of Analysis / Safety Data Sheet

Certificate of Analysis: View current batch

Safety Data Sheet: View Safety Data Sheet

References

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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