An ErbB receptor family inhibitor
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PD 158780

Item No. 13329

Technical Information
Formal Name
N4-(3-bromophenyl)-N6-methyl-pyrido[3,4-d]pyrimidine-4,6-diamine
CAS Number
171179-06-9
Molecular Formula
C14H12BrN5
Formula Weight
Purity
≥98%
A crystalline solid
DMF: 30 mg/mlDMSO: 10 mg/mlEthanol: 2 mg/ml
λmax
226, 312, 404 nm
SMILES
BrC1=CC=CC(NC2=NC=NC3=C2C=C(NC)N=C3)=C1
InChi Code
InChI=1S/C14H12BrN5/c1-16-13-6-11-12(7-17-13)18-8-19-14(11)20-10-4-2-3-9(15)5-10/h2-8H,1H3,(H,16,17)(H,18,19,20)
InChi Key
KFHMLBXBRCITHF-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    PD 158780 is a pyridopyrimidine derivative that reversibly inhibits auto and transphosphorylation of all four members of the ErbB receptor tyrosine kinase superfamily: EGFR (IC50 = 8 µM), ErbB2 (IC50 = 49 nM), ErbB3, and ErbB4 (IC50 = 52 nM).1 It does not inhibit PDGF or FGF-mediated tyrosine phosphorylation.1 At 0.5 µM, PD 158780 has been shown to induce G1 cell cycle arrest in MCF10A breast cancer cells.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Fry, D.W., Nelson, J.M., Slintak, V., et alBiochemical and antiproliferative properties of 4-[Ar(alk)ylamino]pyridopyrimidines, a new chemical class of potent and specific epidermal growth factor receptor tyrosine kinase inhibitor. Biochem. Pharmacol. 54, 877-887 (1997).

    2. Gonzales, A.J., and Fry, D.W. G1 cell cycle arrest due to the inhibition of erbB family receptor tyrosine kinases does not require the retinoblastoma protein. Exp. Cell Res. 303, 56-67 (2005).