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Category: Enzyme-Linked ReceptorsarrowReceptor Tyrosine Kinases (RTKs)arrowEGFR
Cat.No. Product Name
2615 PD 158780
Price and Availability

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PD 158780
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:

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M.Wt: 330.18
Formula: C14H12BrN5
Storage: Store at -20°C
Solubility: Soluble to 100 mM in DMSO and to 25 mM in Ethanol
CAS No: [171179-06-9]

Resources:

  • Certificate of Analysis / MSDS:

    Certificate of Analysis: View current batch
    Product/Material Safety Data Sheet: View current batch

    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. Sun et al (1999) Growth inhibition of nasopharyngeal carcinoma cells by EGF receptor tyrosine kinase inhibitors. Anticancer Res. 19 919. 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.
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    Keywords: PD 158780, Receptor Tyrosine Kinases (RTKs), Potent ErbB Receptor Family Inhibitor, PD158780, Tocris Bioscience

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